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Cancer is one of the leading causes of human death among all major diseases. Metal-based complexes are considered as the most promising vital part in the existing arsenal of cytotoxic candidates used in cancer therapy and diagnostics. The efforts of many scientific groups resulted in the development of numerous metal-based compounds featuring different biologically active organic ligands in order to modulate their bioactivity. Along with the main representatives as potential therapeutic agents, such as the complexes Pt(II)/Pt(IV), Pd(II), Ru(II)/Ru(III), Ag(I), Au(I)/Au(III), Ti(IV), V(IV) and Ga(III), many other transition metal and lanthanide complexes possessing antiproliferative activity are widely discussed in the literature. However, such drugs remain outside the scope of this review. The main purpose of the current study is to review the potential activity of main group metal- and metalloid-based complexes against the most common cancer cell types, such as carcinomas (lung, liver, breast, kidney, gastric, colorectal, bladder, ovarian, cervical, prostate, etc.); sarcomas; blastomas; lymphomas; multiple myeloma; and melanoma. Overcoming the long disregard of organometallic compounds of metals and metalloids from the main groups, a growing number of emerging anticancer agents remarkably prove this field offers an extensive variety of new options for the design of innovative unexplored chemopharmaceutics. Moreover, some of the metal complexes and organometallic compounds from these elements can exhibit entirely different, specific modes of action and biological targets. Obviously, exploitation of their distinct properties deserves more attention. [ABSTRACT FROM AUTHOR]

The RuO2-doped organic polymer composite structure was used as the interface to study the photodiode properties of a Schottky structure. Some basic electrical and optoelectrical parameters of the structure interlaid with RuO2:PVC were investigated using the I–V characteristics in the dark and under definite illuminations. The values of saturation current (I0), barrier height (ΦB0) at zero-bias, ideality factor (n), series and shunt resistances (Rs and Rsh) were calculated by using different methods such as thermionic emission, Ohm's law, Cheung and Norde functions. They were found to be intensely depend on illumination levels and voltage. Forward bias I–V data were used to obtain energy-dependent profiles of interface-states (Nss) for each illumination level. Moreover, the open-circuit voltage (Voc), short circuit current (Isc), filling factor (FF), and efficiency (η) of the fabricated Schottky structure were found as 0.118 V, 6.4 μA, 46%, and 0.088% under 50 mW/cm−2, respectively. According to the findings, the RuO2:PVC organic interlayer is light-sensitive and can thus be used in optoelectronic applications, such as photodetectors and photodiodes. [ABSTRACT FROM AUTHOR]

In this study, to enhance protease production, the wild type of Bacillus subtilis E6-5 was mutagenized by random mutagenesis using ultraviolet radiation and ethidium bromide. After combined treatment, several mutants were obtained. Among these mutants, the mutant strain with the largest proteolytic zone diameter (25 mm) was selected and named Bacillus subtilis ATA38. The enzyme production capacity of the obtained mutant was tested and the mutant strain (404 IU/mL at 24 hours) produced 6.7 times more enzyme than the parental strain (60 IU/mL at 32 hours). The effects of some important parameters in the growth medium on enzyme production were examined. The best carbon, organic nitrogen and metal ion were obtained with wheat starch (525 IU/mL), meat extract (850 IU/mL) and KCl+CaCl2 (548 IU/mL), respectively. pH 6.0, 37°C, 200 rpm, inoculum age 18 hours and inoculation amount 1% were obtained as the best physical factors. To further increase the yield, the best nutritional and physical parameters were combined to create a new modified medium. It was determined that the enzyme yield with mutant strain increased 2.7 times in the modified medium (1096 IU/mL) compared to the control (404 U/mL). The mutant strain (1096 IU/mL) showed an 18.2-fold increase in production compared to the wild type (60 IU/mL) in the modified medium. Protease enzyme obtained from ATA38 mutant strain may have great potential in industry for different purposes. [ABSTRACT FROM AUTHOR]

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Magnetic nanoparticle–incorporated metal organic frameworks (MOF) are potential composites for various applications such as catalysis, water treatment, drug delivery, gas storage, chemical sensing, and heavy metal ion removal. MOFs exhibits high porosity and flexibility enabling guest species like heavy metal ions to diffuse into bulk structure. Additionally, shape and size of the pores contribute to selectivity of the guest materials. Incorporation of magnetic materials allows easy collection of adsorbent materials from solution system making the process simple and cost-effective. In view of the above advantages in the present review article, we are discussing recent advances of different magnetic material–incorporated MOF (Mg-MOF) composite for application in photocatalytic degradation of dyes and toxic chemicals, adsorption of organic compounds, adsorption of heavy metal ions, and adsorption of dyes. The review initially discusses on properties of Mg-MOF, different synthesis techniques such as mechanochemical, sonochemical (ultrasound) synthesis, slow evaporation and diffusion methods, solvo(hydro)-thermal and iono-thermal method, microwave-assisted method, microemulsion method post-synthetic modification template strategies and followed by application in waste water treatment. [ABSTRACT FROM AUTHOR]

Low-cost and safe batteries are considered to be promising energy-storage systems. Here, a metal organic framework (MOF)-derived octahedral Cu1.95S@CoS2 composite is developed as a high-performance cathode of aluminium-ion (Al-ion) batteries. CoS2 nanoparticles on Cu1.95S provide active sites, making AlCl4− intercalation/deintercalation highly reversible, and reducing polarization. Cycling at 0.5 A g−1, Cu1.95S@CoS2 maintains stable capacities of 136.6 and 122.4 mA h g−1 after 200 cycles at room temperature and −10 °C, respectively. Stable rate-performance is also achieved. These findings will accelerate the application of Al-ion batteries and MOF-derived energy-storage composites. [ABSTRACT FROM AUTHOR]

The reaction of the Ag(I) dimer [Ag2(η2-A)2(μ,η1:η1-A)2][TEF]2 (A = [{CpMo(CO)2}2(μ,η2-P2)]) possessing labile η2-coordinated P2 ligands with the organometallic dipnictogen compounds [{CpMo(CO)2}2(μ,η2-EE′)] (E = E′ = As, Sb; E = P, E′ = As, Sb) represents a facile synthetic route towards unprecedented heteroleptic pnictogen-rich supramolecular complexes. This method can also be extended to the analogous Cu(I) dimer and is studied by DFT computations. [ABSTRACT FROM AUTHOR]

The achievement of significant photoluminescence (PL) in lanthanide ions (Ln3+) has primarily relied on host sensitization, where energy is transferred from the excited host material to the Ln3+ ions. However, this luminous mechanism involves only one optical antenna, namely the host material, which limits the accessibility of excitation wavelength‐dependent (Ex‐De) PL. Consequently, the wider application of Ln3+ ions in light‐emitting devices is hindered. In this study, we present an organic–inorganic compound, (DMA)4LnCl7 (DMA+=[CH3NH2CH3]+, Ln3+=Ce3+, Tb3+), which serves as an independent host lattice material for efficient Ex‐De emission by doping it with trivalent antimony (Sb3+). The pristine (DMA)4LnCl7 compounds exhibit high luminescence, maintaining the characteristic sharp emission bands of Ln3+ and demonstrating a high PL quantum yield of 90–100 %. Upon Sb3+ doping, the compound exhibits noticeable Ex‐De emission with switchable colors. Through a detailed spectral study, we observe that the prominent energy transfer process observed in traditional host‐sensitized systems is absent in these materials. Instead, they exhibit two independent emission centers from Ln3+ and Sb3+, each displaying distinct features in luminous color and radiative lifetime. These findings open up new possibilities for designing Ex‐De emitters based on Ln3+ ions. [ABSTRACT FROM AUTHOR]

Directional defects management in polycrystalline perovskite film with inorganic passivator is highly demanded while yet realized for fabricating efficient and stable perovskite solar cells (PSCs). Here, we develop a directional passivation strategy employing a two‐dimensional (2D) material, Cu‐(4‐mercaptophenol) (Cu‐HBT), as a passivator precursor. Cu‐HBT combines the merits of the targeted modification from organic passivator and excellent stability offered by inorganic passivator. Featuring with dense organic functional motifs on its surfaces, Cu‐HBT has the capability to "find" and fasten to the Pb defect sites in perovskites through coordination interactions during a spin‐coating process. During subsequent annealing treatment, the organic functional motifs cleave from Cu‐HBT and convert in situ into p‐type semiconductors, Cu2S and PbS. The resultant Cu2S and PbS not only serve as stable inorganic passivators on the perovskite surface, significantly enhancing cell stability, but also facilitate efficient charge extraction and transport, resulting in an impressive efficiency of up to 23.5 %. This work contributes a new defect management strategy by directionally yielding the stable inorganic passivators for highly efficient and stable PSCs. [ABSTRACT FROM AUTHOR]

In this study, toxicity of zeolitic metal organic framework-8 nanoparticles on the growth of Escherichia coli, Pseudomonas aeruginosa and Staphylococcus aureus at concentrations of 5–2500 mg/L was assessed. The data were analysed using the Probit analysis and the values of no observed effect concentration (NOEC), lethal concentration-50 (LC50) and 100% bacterial growth inhibition were determined. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) were quantified by micro-dilution method. The 24-h LC50 was 435.24, 327.08 and 76.54 mg/L and NOEC was 147.59, 103.851 and 25.662 mg/L for E. coli, P. aeruginosa and S. aureus, respectively. The 100% growth inhibitory as observed at 2009.093, 1657.094 and 359.833 mg/L, for E. coli, P. aeruginosa and S. aureus, respectively. The lowest MIC and MBC were 12.98 and 26.04 mg/L for S. aureus. This study showed that S. aureus was the suitable indicator due to its high sensitivity to zeolitic metal organic framework-8. [ABSTRACT FROM AUTHOR]

The published data on the substituent influence on the boiling points Tb for 19 series of boron, aluminium, silicon, germanium, tin, and phosphorus compounds were considered using correlation analysis. It was established for the first time that the Tb values depend not only on the classical (inductive, resonance, and steric) effects, but also on the polarizability effect of substituents. In some series, the polarizability effect has a major influence on Tb. [ABSTRACT FROM AUTHOR]

Purpose: Pollution of the environment with all kinds of plastics has become a growing problem. The problem of microplastics is mainly due to the absorption of stable organic pollutants and metals into them, and as a result, their environmental toxicity increases. The main purpose of this study is to investigate the appropriate and efficient methods of removing microplastics from aqueous environments through a systematic review. Methods: Present study designed according to PRISMA guidelines. Two independent researchers followed all process from search to final analysis, for the relevant studies using international databases of PubMed, Scopus and ISI/WOS (Web of Science), without time limit. The search strategy developed based on the main axis of "microplastics", "aqueous environments" and "removal". This research was carried out from 2017 until the March of 2022. All relevant observational, analytical studies, review articles, and a meta-analysis were included. Results: Through a comprehensive systematic search we found 2974 papers, after running the proses of refining, 80 eligible papers included to the study. According to the results of the review, the methods of removing microplastics from aquatic environments were divided to physical (12), chemical (18), physicochemical (27), biological (12) and integrated (11) methods. In different removal methods, the most dominant group of studied microplastics belonged to the four groups of polyethylene (PE), polystyrene (PS), polypropylene (PP) and polyethylene tetra phthalate (PET). Average removal efficiency of microplastics in different processes in each method was as: physical method (73.76%), chemical method (74.38%), physicochemical method (80.44%), biological method (75.23%) and integrated method (88.63%). The highest removal efficiency occurred in the processes based on the integrated method and the lowest efficiency occurred in the physical method. In total, 80% of the studies were conducted on a laboratory scale, 18.75% on a full scale and 1.25% on a pilot scale. Conclusion: According to the findings; different processes based on physical, chemical, physicochemical, biological and integrated methods are able to remove microplastics with high efficiency from aqueous environments and in order to reduce their hazardous effects on health and environment, these processes can be easily used. [ABSTRACT FROM AUTHOR]

The extraction of U(VI), Th(IV), Am(III), and lanthanides(III) from nitric acid solutions with solutions of phosphorylated pyrazines in organic solvents was studied. The stoichiometry of the extracted complexes was determined, and the influence of the structure of the extractant and an HNO3 concentration in the aqueous phase on the efficiency of the extraction of metal ions into the organic phase was considered. It was established that among the studied compounds, bis(diphenylphosphine)quinoxaline dioxide has the highest extraction ability with respect to actinides and lanthanides in nitric acid media. [ABSTRACT FROM AUTHOR]

A convenient synthesis of [HB(HImMe)3](PF6)2 (ImMe = N-methylimidazolyl) is decribed. This salt serves in situ as a precursor to the tris(imidazolylidenyl)borate Li[HB(ImMe)3] pro-ligand upon deprotonation with nBuLi. Reaction with [W(≡CC6H4Me-4)(CO)2(pic)2(Br)] (pic = 4-picoline) affords the carbyne complex [W(≡CC6H4Me-4)(CO)2{HB(ImMe)3}]. Interrogation of experimental and computational data for this compound allow a ranking of familiar tripodal and facially coordinating ligands according to steric (percentage buried volume) and electronic (νCO) properties. The reaction of [W(≡CC6H4Me-4)(CO)2{HB(ImMe)3}] with [AuCl(SMe2)] affords the heterobimetallic semi-bridging carbyne complex [WAu(μ-CC6H4Me-4)(CO)2(Cl){HB(ImMe)3}]. [ABSTRACT FROM AUTHOR]

Cambridge Structural Database (CSD) is the largest repository of crystal data, containing over 1.2 million crystal structures of organic, metal–organic and organometallic compounds. It is a powerful research tool in many areas, including the extensive studying of noncovalent interactions. In this review, we show how a thorough analysis of CSD crystal data resulted in recognition of novel types of stacking interactions. Even though stacking interactions were traditionally related to aromatic systems, a number of crystallographic studies have shown that nonaromatic metal–chelate rings, as well as hydrogen-bridged rings, can also form stacking interactions. Joined efforts of a CSD analysis and quantum chemical calculations showed that these new stacking interactions are stronger than stacking interactions of aromatic species and recognized them as very important attractive forces in numerous supramolecular systems. [ABSTRACT FROM AUTHOR]

Sustainable water desalination and purification membrane processes require new practical pathways to improve their efficiency. To this end, the inclusion of two-dimensional materials in membrane structure has proven to have a significant impact in various applications. In particular, in processes such as membrane distillation and crystallization, these materials, thanks to their characteristics, help to increase the recovery of clean water and, at the same time, to improve the quality and the production of the recovered salts. Therefore, a fundamental aspect of obtaining 2D materials with certain characteristics is the technique used for the preparation. This review provides a broad discussion on the preparation and proprieties of 2D materials, including examples of organic structures (such as graphene and structures containing transition metals and organic metals). Finally, the critical challenges, future research directions, and the opportunities for developing advanced membranes based on 2D materials are outlined. [ABSTRACT FROM AUTHOR]

AbstractNeuroendocrine tumors (NETs) are rare, diverse malignancies; approximately two thirds originate in the gastrointestinal tract and pancreas and are known as gastroenteropancreatic NET. Most cases are diagnosed in the advanced or metastatic setting and overexpress somatostatin receptors. Recommended first-line treatment is somatostatin analogs; however, disease progression is common. [177Lu]Lu-DOTA-TATE is a radiolabeled peptide receptor radionuclide therapy (PRRT) indicated for the treatment of adult patients with somatostatin receptor-positive foregut, midgut, and hindgut gastroenteropancreatic NETs and progression on first-line somatostatin analogs. Many primary oncology practices may lack the staff, expertise, and infrastructure to treat patients with PRRT and primary oncologists may therefore refer their patients to a NET specialist at a tertiary center for treatment. Given the amount of organization required, PRRT treatment may seem to be complex; however, this process will be managed by a care coordinator who acts as a consistent point of contact for primary physicians regarding the care of their patients and ensures blood tests and scans are scheduled. In this article, we share our opinions, procedures, workflow, best practice, and roles and responsibilities when caring for patients receiving [177Lu]Lu-DOTA-TATE and focus on the role of the primary oncologist before, during, and after PRRT treatment.

68Ga-satoreotide trizoxetan is a novel somatostatin receptor antagonist associated with high sensitivity and reproducibility in neuroendocrine tumor (NET) detection and localization. However, the optimal peptide mass and radioactivity ranges for 68Ga-satoreotide trizoxetan have not yet been established. We therefore aimed to determine its optimal dosing regimen in patients with metastatic gastroenteropancreatic NETs in a prospective, randomized, 2 × 3 factorial, multicenter phase II study. Methods: Patients received 68Ga-satoreotide trizoxetan at a peptide mass of 5-20 µg on day 1 of the study and of 30-45 µg on days 16-22, at 1 of 3 68Ga radioactivity ranges (40-80, 100-140, or 160-200 MBq). Whole-body PET/CT imaging was performed 50-70 min after each injection. The primary endpoint was the detection rate of NET lesions imaged by 68Ga-satoreotide trizoxetan relative to contrast-enhanced CT (for each of the 6 peptide mass and radioactivity range combinations). Results: Twenty-four patients were evaluated in the per-protocol analysis. The median number of lesions detected by 68Ga-satoreotide trizoxetan PET/CT or PET alone was at least twice as high as the number detected by contrast-enhanced CT across the 6 studied peptide mass and radioactivity range combinations. There were no differences between the 2 peptide mass ranges or between the 3 radioactivity ranges in the number of identified lesions. However, a trend toward a lower relative lesion count was noted in the liver for the 40- to 80-MBq range. No relationship was observed between the radioactivity range per patient's body weight (MBq/kg) and the number of lesions detected by 68Ga-satoreotide trizoxetan. The median diagnostic sensitivity of 68Ga-satoreotide trizoxetan PET/CT, based on the number of lesions per patient, ranged from 85% to 87% across the different peptide mass and radioactivity ranges. Almost all reported adverse events were mild and self-limiting. Conclusion: A radioactivity of 100-200 MBq with a peptide mass of up to 50 µg was confirmed as the optimal dosing regimen for 68Ga-satoreotide trizoxetan to be used in future phase III studies.

BackgroundGadofosveset is a gadolinium-based blood pool contrast agent that was approved by the United States Food and Drug Administration in 2008. Its unanticipated withdrawal from production in 2016 created a void in the blood pool agent inventory and highlighted the need for an alternative agent with comparable imaging properties.ObjectiveThe purpose of our study is to compare the diagnostic image quality, vascular contrast-to-noise ratio (CNR) and temporal signal characteristics of gadofosveset trisodium and ferumoxytol at similar molar doses for high-resolution, three-dimensional (3-D) magnetic resonance (MR) venography in children.Materials and methodsThe medical records and imaging data sets of patients who underwent high-resolution 3-D gadofosveset-enhanced MR venography (GE-MRV) or ferumoxytol-enhanced MR venography (FE-MRV) were retrospectively reviewed. Two groups of 20 pediatric patients (age- and weight-matched with one patient common to both groups; age range: 2 days-15 years) who underwent high-resolution 3-D GE-MRV or FE-MRV at similar molar doses were identified and analyzed. Qualitative analysis of image quality and vessel definition was performed by two blinded pediatric radiologists. Interobserver agreement was assessed with the AC1 (first-order agreement coefficient) statistic. Signal-to-noise ratio (SNR) and CNR of the inferior vena cava and aorta were measured in the steady-state venous phase. Medical records were retrospectively reviewed for any adverse reactions associated with either contrast agent.ResultsMeasured SNR and CNR of the inferior vena cava were higher for FE-MRV than GE-MRV (P = 0.034 and P

The biosynthesis of the active site of the [FeFe]-hydrogenases (HydA1), the H-cluster, is of interest because these enzymes are highly efficient catalysts for the oxidation and production of H2. The biosynthesis of the [2Fe]H subcluster of the H-cluster proceeds from simple precursors, which are processed by three maturases: HydG, HydE, and HydF. Previous studies established that HydG produces an Fe(CO)2(CN) adduct of cysteine, which is the substrate for HydE. In this work, we show that by using the synthetic cluster [Fe2(μ-SH)2(CN)2(CO)4]2- active HydA1 can be biosynthesized without maturases HydG and HydE.

An in-depth study of the mechanism of the azidation of C(sp3)-H bonds with Zhdankin's λ3-azidoiodane reagent catalyzed by iron(II)(pybox) complexes is reported. Previously, it was shown that tertiary and benzylic C(sp3)-H bonds of a range of complex molecules underwent highly site-selective azidation by reaction with a λ3-azidoiodane reagent and an iron(II)(pybox) catalyst under mild conditions. However, the mechanism of this reaction was unclear. Here, a series of mechanistic experiments are presented that reveal critical features responsible for the high selectivity and broad scope of this reaction. These experiments demonstrate the ability of the λ3-azidoiodane reagent to undergo I-N bond homolysis under mild conditions to form λ2-iodanyl and azidyl radicals that undergo highly site-selective and rate-limiting abstraction of a hydrogen atom from the substrate. The resultant alkyl radical then combines rapidly with a resting state iron(III)-azide complex, which is generated by the reaction of the λ3-azidoiodane with the iron(II)(pybox) complex, to form the C(sp3)-N3 bond. This mechanism is supported by the independent synthesis of well-defined iron complexes characterized by cyclic voltammetry, X-ray diffraction, and EPR spectroscopy, and by the reaction of the iron complexes with alkanes and the λ3-azidoiodane. Reaction monitoring and kinetic studies further reveal an unusual effect of the catalyst on the rate of formation of product and consumption of reactants and suggest a blueprint for the development of new processes leading to late-stage functionalization of C(sp3)-H bonds.

BACKGROUND: Neonates and young children require efficacious magnetic resonance imaging (MRI) examinations but are potentially more susceptible to the short- and long-term adverse effects of gadolinium-based contrast agents due to the immaturity of their body functions. OBJECTIVE: To evaluate the acute safety and diagnostic efficacy of gadoteridol (ProHance) for contrast-enhanced MRI of the central nervous system (CNS) in children ≤2 years of age. MATERIALS AND METHODS: One hundred twenty-five children ≤2 years old (including 57 children

Relevance. The problem of studying organometallic compounds in carbonized and carbonaceous substances is part of the global problem of the structure of natural materials from plant remains and manifestation of ore genesis in organic sedimentary deposits. This problem covers a number of issues. The most pressing one among them is the form of occurrence of finely dispersed gold in the form of organometallic compounds in metal-bearing coals and shales. This is especially true for large gold deposits of black shale strata. Aim. To study the relationship between sedimentation of organic formations and ore genesis in black shale deposits using the example of the Verninskoe deposit (Patom Highlands, Yakutia). Using the SKAUFV hardware and software complex together with ICP-MS and INAA methods, which allow one to assess the degree of Au concentration in organic matter, to substantiate the possibility of determining organometallic compounds of gold that are significant in the processes of sedimentogenesis, lithogenesis and epigenesis. Methods. IR spectroscopy, instrumental neutron activation analysis (INAA) and inductively coupled plasma mass spectrometry (ICP-MS). Results. The authors have determined that the SKAUFV hardware and software complex, together with the ICP-MS and INAA methods, makes it possible to establish the role of organic matter in metasomatism and to identify temperature zonality and the associated gold concentration in the ore zone. To determine the organometallic compounds of Au, structural and genetic indicators (Pm, Ko, PVt+L, PI) were selected. These indicators reflect the significance of sedimentation, diagenesis, catagenesis and epigenesis on Au concentration of in organic matter. These indicators made it possible to assess the level of temperature impact on sedimentary deposits of regional metamorphism and near-ore metasomatism. In this regard, subzones of Au concentration were established in the ore zone, determined by temperature zoning in the form of a manifestation of local metasomatism. The latter was influenced by the protein-fat composition of plants that form organic matter.

Transition metals are well known for their catalytic behaviours for the activation of the Carbon-Carbon (C-C) bond. Many chemists have created various important developments in this field during the last decades. In the present review, only a few instances of catalytic activation of the C-C bond using the transition metal catalyst and their mechanism have been disclosed, which is useful information for creating new ways to break these bonds. This review includes the recent advances in the activation of cyclic, saturated and unsaturated carbon–carbon bonds utilizing transition metals as a catalyst in a number of different systems.

The controlled synthesis of metal organic nanosheets (MONs) still remains a challenge for scientists and is of primary interest in many research areas. In this study, we have developed a simple and reproducible one-pot synthesis method leading to tunable cobalt-based hybrid materials consisting of nanosheets with a well-defined morphology. The synthesis is performed via a solvothermal process assisted by primary amines acting as surfactants. The obtained materials are composed of ultrathin nanosheets with a rectangular morphology (width of about 50 nm and length greater than 100 nm). The different analysis techniques used show that the nanosheets are constituted by the alternation, in their width, of inorganic fringes (cobalt hydroxide) and organic ones (dicarboxylic acid) and that amine molecules stabilize their surface. 3D organisation of the nanosheets can be achieved at a synthesis temperature above 190 °C due to the interaction of alkyl chains of the stabilising amines. A multiparametric study based on SAXS experiments and TEM and PXRD analyses has highlighted the control of structural parameters by variations of some synthesis conditions. The inter-fringe distances are tunable from 1.0 nm to 1.5 nm through the length of the dicarboxylic linker and the distances between nanosheets can be modulated by the length of the alkyl chain of the primary amines. This efficient one-pot process seems to be very promising for the synthesis of tunable multiscale nanostructured MONs and can be implemented in many research areas, opening the way for various applications. [ABSTRACT FROM AUTHOR]

Metal nanoparticle-organic interfaces are common but remain elusive for controlling reactions due to the complex interactions of randomly formed ligand-layers. This paper presents an approach for enhancing the selectivity of catalytic reactions by constructing a skin-like few-nanometre ultrathin crystalline porous covalent organic overlayer on a plasmonic nanoparticle surface. This organic overlayer features a highly ordered layout of pore openings that facilitates molecule entry without any surface poisoning effects and simultaneously endows favourable electronic effects to control molecular adsorption–desorption. Conformal organic overlayers are synthesised through the plasmonic oxidative activation and intermolecular covalent crosslinking of molecular units. We develop a light-operated multicomponent interfaced plasmonic catalytic platform comprising Pd-modified gold nanoparticles inside hollow silica to achieve the highly efficient and selective semihydrogenation of alkynes. This approach demonstrates a way to control molecular adsorption behaviours on metal surfaces, breaking the linear scaling relationship and simultaneously enhancing activity and selectivity. Controlling molecular interactions on metal surfaces for selective chemical synthesis remains difficult to achieve. Here, we report thin, porous covalent organic overlayers on metal nanocrystals to improve selectivity through plasmonic activation. [ABSTRACT FROM AUTHOR]

Tetraphenylethylenes (TPEs) are well-known for their aggregation-induced emission properties. The synthesis of TPE derivatives, as well as other highly substituted olefins, generally requires the use of hazardous reagents, such as metalorganic compounds, to overcome the high activation energies caused by the sterically congested double bond. Herein, we present an efficient and metal-free procedure for the synthesis of tetraarylethylenes via alkylidene-homocoupling of N-tosylhydrazones, derived from readily available benzophenones, in excellent yields. The method relies only on cheap and benign additives, i.e. elemental sulfur and potassium carbonate, and easily competes with other established procedures in terms of scope, yield and practicability. A mechanistic study revealed a diazo compound, a thioketone and a thiirane as key intermediates in the pathway of the reaction. Based on this, a modified method, which allows for selective alkylidene-cross-coupling, generating a broader scope of tri- and tetrasubstituted olefins in good yields, is showcased as well. Tetraphenylethylenes (TPEs) are known for their aggregation-induced emission and electrochemical properties of value for optical sensors, however, established synthetic routes suffer from several limitations. Here, the authors develop a metal-free route to TPEs and other alkenes via a sulfur-mediated coupling of N-tosylhydrazones, achieving good yields and a broad substrate scope. [ABSTRACT FROM AUTHOR]

Colloidal lead halide perovskites face challenges in practical optoelectronic applications due to the toxicity of lead (II). To overcome this issue, a novel approach using metal‐organic frameworks (MOFs) for recycling lead (II) management in perovskite materials, is developed. Through surface‐functionalization of MOF‐808 and pH tuning, the MOF achieves recyclable adsorption‐desorption of lead (II), confining the lead source within the MOF‐808 template or the perovskites. This controllable transformation between lead (II) chelation and perovskites prevents lead (II) leakage. Additionally, separated lead (II) ions from decomposed perovskite can be adsorbed by MOF‐808, facilitating recycling. The resulting MOF‐808‐EDTA@CsPbBr3 composite exhibits comparable optical performance to pure CsPbBr3 powder, but with improved stabilities, effectively preventing lead (II) leakage. Hierarchical desorption of lead (II) in the MOF‐808‐EDTA@Pb2+ complex enables reversible on/off fluorescence signal switching. Detached lead (II) from decomposed MOF‐808‐EDTA@CsPbBr3 composite can be re‐adsorbed by MOF‐808‐EDTA, enabling the construction of CsPbBr3 nanocrystals in a new cycle. This approach is economically attractive and environmentally friendly. This study addresses the challenge of lead (II) leakage and offers the potential for optical anti‐counterfeiting in perovskite materials with a sustainable approach. [ABSTRACT FROM AUTHOR]

[Display omitted] Exploitation of solid-state proton-conducting materials with high anhydrous proton conductivity from subzero temperature (<273 K) to moderate temperature (>353 K) is a great challenge. Here, Brönsted acid-dopped zirconium-organic xerogels (Zr/BTC-xerogels) are prepared for anhydrous proton conduction from subzero to moderate temperature. Abundant acid sites and strong H-bonding interactions make the CF 3 SO 3 H (TMSA)-introduced xerogel gain high proton conductivity from 9.0 × 10-4 S cm−1 (253 K) to 1.40 × 10-2 S cm−1 (363 K) under anhydrous conditions, which are in the leading level. This provides a new possibility to develop wide-operating-temperature conductors. [ABSTRACT FROM AUTHOR]

While R2C=N−R double bonds in organic imines are well established, the related iminoboranes R‐B=N−R are either prone to oligomerization or can only be stabilized at sufficient steric congestion. In particular, the examples of unsubstituted parent B=N‐H entity are rare. We demonstrate that the amino imidazoline‐2‐imine ligand system (HAmIm) not only gives rise to the isolation of a parent (AmIm)B=N−H iminoborane, but also to species of type (AmIm)B=N‐SiMe3 with concomitant stabilization by lithium bromide. The double bond character in these systems is unambiguously corroborated by DFT calculations. The steric accessibility of the (AmIm)B=NH unit allows facile reactivity including metathesis reactions with C=O and C=S bonds, nucleophilic addition toward organic and organometallic carbonyl compounds, but also oxidative N−N coupling within a dimeric unit. Thus, the chemical behavior of the (AmIm)B=N−H and (AmIm)B=N‐SiMe3 is distinctly different from that of organic imines. [ABSTRACT FROM AUTHOR]

A series of four regioisomeric Pt(II) complexes (PtLa-n and PtLb-n) bearing tetradentate luminophores as dianionic ligands were synthesized. Hence, both classes of cyclometallating chelators were decorated with three n-hexyl (n = 6) or n-dodecyl (n = 12) chains. The new compounds were unambiguously characterized by means of multiple NMR spectroscopies and mass spectrometry. Steady-state and time-resolved photoluminescence spectroscopy as well quantum chemical calculations show that the effect of the regioisomerism on the emission colour and on the deactivation rate constants can be correlated with the participation of the Pt atom on the excited state. The thermal properties of the complexes were studied by DSC, POM and temperature-dependent steady-state photoluminescence spectroscopy. Three of the four complexes (PtLa-12, PtLb-6 and PtLb-12) present an intriguing thermochromism resulting from the responsive metal–metal interactions involving adjacent monomeric units. Each material has different transition temperatures and memory capabilities, which can be tuned at the intermolecular level. Hence, dipole–dipole interactions between the luminophores and disruption of the crystalline packing by the alkyl groups are responsible for the final properties of the resulting materials. [ABSTRACT FROM AUTHOR]

The effective storage and utilization of hydrogen energy is expected to solve the problems of energy shortage and environmental pollution currently faced by human society. Metal–organic framework materials (MOFs) have been shown by scientists to be very potential hydrogen storage materials. However, the current design methods and strategies for MOFs are still generally in the trial‐and‐error stage, and the research works are at the overall level. To solve the problems of directional design and rational construction of new MOFs, this work uses the principles and methods of coordination chemistry and crystal engineering to carry out the theoretical design and mechanism research of new MOFs for high‐efficiency hydrogen storage application scenarios. In this study, the structures selected for theoretical calculation were divided into two types: different ligands for the same metal (IRMOFs, MOF‐205, and DUT‐23‐Zn) and different metals for the same ligand (DUT‐23‐M [(M = Co, Ni, Cu, and Zn]). The model construction process, hydrogen loading with temperature, specific surface area, hydrogen adsorption energy, charge density and hydrogen storage mechanism of the above structures were analyzed, and the key indicators that may affect the hydrogen storage performance of MOFs were summarized: type and quantity of coordination metals, temperature, pressure, adsorption site and specific surface area. [ABSTRACT FROM AUTHOR]

Metal carbonyl complexes possess among the most storied histories of any compound class in organometallic chemistry. Nonetheless, these old dogs continue to be taught new tricks. In this Feature, we review the historic discoveries and recent advances in cleaving robust bonds (e.g., C–H, C–O, C–F) using carbonyl complexes of three metals: Mn, Fe, and Co. The use of Mn, Fe, and Co carbonyl catalysts in controlling selectivity during hydrofunctionalization reactions is also discussed. The chemistry of these earth-abundant metals in the field of robust bond functionalization is particularly relevant in the context of sustainability. We expect that an up-to-date perspective on these seemingly simple organometallic species will emphasize the wellspring of reactivity that continues to be available for discovery. [ABSTRACT FROM AUTHOR]

Dynamic covalent chemistry (DCvC) is a powerful and widely applied tool in modern synthetic chemistry, which is based on the reversible cleavage and formation of covalent bonds. One of the inherent strengths of this approach is the perspective to reversibly generate in an operationally simple approach novel structural motifs that are difficult or impossible to access with more traditional methods and require multiple bond cleaving and bond forming steps. To date, these fundamentally important synthetic and conceptual challenges in the context of DCvC have predominantly been tackled by exploiting compounds of lighter p‐block elements, even though heavier p‐block elements show low bond dissociation energies and appear to be ideally suited for this approach. Here we show that a dinuclear organometallic bismuth compound, containing BiMe2 groups that are connected by a thioxanthene linker, readily undergoes selective and reversible cleavage of its Bi−C bonds upon exposure to external stimuli. The exploitation of DCvC in the field of organometallic heavy p‐block chemistry grants access to unprecedented macrocyclic and barrel‐type oligonuclear compounds. [ABSTRACT FROM AUTHOR]

Topoisomerases are interesting targets in cancer chemotherapy. Here, we describe the design and synthesis of a novel copper(II) indenoisoquinoline complex, WN198. The new organometallic compound exhibits a cytotoxic effect on five adenocarcinoma cell lines (MCF-7, MDA-MB-231, HeLa, HT-29, and DU-145) with the lowest IC50 (0.37 ± 0.04 μM) for the triple-negative MDA-MB-231 breast cancer cell line. Below 5 µM, WN198 was ineffective on non-tumorigenic epithelial breast MCF-10A cells and Xenopus oocyte G2/M transition or embryonic development. Moreover, cancer cell lines showed autophagy markers including Beclin-1 accumulation and LC3-II formation. The DNA interaction of this new compound was evaluated and the dose-dependent topoisomerase I activity starting at 1 μM was confirmed using in vitro tests and has intercalation properties into DNA shown by melting curves and fluorescence measurements. Molecular modeling showed that the main interaction occurs with the aromatic ring but copper stabilizes the molecule before binding and so can putatively increase the potency as well. In this way, copper-derived indenoisoquinoline topoisomerase I inhibitor WN198 is a promising antitumorigenic agent for the development of future DNA-damaging treatments. [ABSTRACT FROM AUTHOR]

The number of cartilaginous fish is declining worldwide and contaminants are one of the primary stress factors in marine organisms. The spinetail devil ray or giant devil ray (Mobula mobular) is listed as an 'Endangered species' globally in the IUCN Red List of Threatened Species. One individual devil ray caught in Saronikos Gulf was tested for trace metals (Zn, Cu, Fe, Mn, Ni, Cr, Pb and Hg) and organochlorine contaminants (PCBs and DDTs). The concentrations of contaminants in the muscle tissue of the devil ray did not exceed safe human consumption limits. However, relatively elevated levels of trace metals and PCBs were measured in the liver and in particular the PCB congeners were five times higher than the European Commission limit. This study highlights the need for future research on the potential impacts of trace metals and organic contaminants on elasmobranchs and more specifically on threatened species. [ABSTRACT FROM AUTHOR]

Recently, proteins separation has drawn great interest for the full investigation of a proteome because the proteins separation is the precondition when conducting clinical research or proteomics research. Metal organic frameworks (MOFs) are fabricated via covalent connection between organic ligands and metal ions/clusters units. MOFs have attracted much attention due to the ultra-high specific surface area, tunable structure, more metal site or unsaturated site, and chemical stability. Over the past decade, different functionalization types of MOFs have been reported in combination with amino acids, nucleic acids, proteins, polymers, and nanoparticles for various applications. In this review, the synthesis and functionalization of MOFs have been thoroughly discussed, and we introduced the existing problems and development trends in these fields. Furthermore, MOFs as advanced adsorbents for selective separation of proteins/peptides are summarized. Additionally, we present a comprehensive prospects and challenges in the preparation of robust functional MOFs-based adsorbents and make a final outlook on their future development prospects in selective separation of proteins/peptides. [ABSTRACT FROM AUTHOR]

The sustained and controlled delivery of antimicrobial drugs has been largely studied using nanomaterials, like metal organic frameworks (MOFs), and various polymers. However, not much attention has been given to combining MOFs and biodegradable polymers towards the potentially more sustained release of active pharmaceutical ingredients. Herein, we report a comparative study of two widely used antimicrobial drugs, cephalexin and metronidazole, from zinc-based MOF-5 incorporated into biodegradable polycaprolactone (PCL) and poly-lactic glycolic acid (PLGA) composites. Cephalexin and metronidazole were separately loaded into MOF-5 post-synthetically, followed by their integration into biodegradable PLGA and PCL composites. The pristine MOF-5 and the loaded MOFs were thoroughly characterised using Fourier-transformed infrared (FT-IR) spectroscopy, scanning electron microscopy (SEM), thermogravimetric analysis (TGA) and powder X-ray diffraction (PXRD). Ultraviolet-visible (UV-Vis) spectroscopy studies were carried out to assess the release of the drugs in PBS for up to 72 h, showing a cumulative release of 24.95 wt% and 27.84 wt% for cephalexin and metronidazole, respectively. The antibacterial properties of the pristine MOF, pure drugs, drug-loaded MOFs and the loaded composites were assessed against Gram-positive and Gram-negative bacterial strains, Staphylococcus aureus or Staphylococcus epidermidis and Escherichia coli or Acinetobacter baumanii, respectively. A cephalexin-loaded MOF-5 composite of PCL (PCL-ceph@MOF-5) showed the best efficiency for the controlled release of drugs to inhibit the growth of the bacteria compared to the other composites. This study demonstrates that the combination of MOFs with biodegradable polymers can provide an efficient platform for the sustained release of antimicrobial drugs and can be a promising tool to manage antimicrobial resistance (AMR). [ABSTRACT FROM AUTHOR]

In order to solve the problem of low redox ability and high recombination rate of photogenerated carriers in the system of simultaneous elimination of heavy metals and organic pollutant, UiO-66/MoS2 composite (0.2MoUiO) with the best catalytic performance was synthesized by one-step solvothermal method using MoS2 as cocatalyst and adjusting the amount of MoS2. 0.2MoUiO was used for synergistic photocatalytic removal of Cr(VI) and methylene blue (MB). In this experiment, the concentration of MB and Cr(VI) was 5 mg/L, the amount of catalyst was 0.1 g/L, 0.2MoUiO can concurrently remove 98% of MB and 90% Cr( under visible light irradiation in 80 min. The photocatalytic degradation rate of MB over 0.2MoUiO was 1.89 times higher than those single system of MB. Meanwhile, the reduction rate of Cr(VI) over 0.2MoUiO reached 2.87 times compared with it. The enhanced performance is attributed to that Z-scheme heterojunction formed between UiO-66 and MoS2, which enhanced light absorption capacity by 0.2MoUiO and accelerates the separation of electrons and holes, It was verified by PL, XPS valence band test and UV-vis DRS. • OH and • O2- was the main active substance of the photocatalyst of MB by mechanism and ESR test analysis, and the process of synergistic degradation of Cr(VI), MB could act as a sacrificial agent to effectively consume h+ and • O2-, then promote electron accumulation, which was conducive to reducing Cr(VI). [ABSTRACT FROM AUTHOR]

Carbon dioxide emission into the atmosphere, which originates from fossil fuels consumption, has led to a serious environmental and energy crisis. Electrochemical CO2 reduction reaction (CO2RR) into valuable chemicals such as carbon monoxide, ethanol, ethylene, and methane not only help lower the CO2 concentration in the atmosphere but is also beneficial for sustainable energy production. Therefore, numerous works are assigned to improving efficient electrocatalytic materials for the selective CO2RR. Metal–organic framework (MOF)‐derived catalytic materials mostly based on transition metals demonstrate permissible CO2RR owing to their specific composition, tunable surface nanostructure and texture, and affordable market prices. In this work, the best effort is put to describe the most basic concept of electrochemical CO2RR to provide a consensus. The effect of MOF structure and surface analysis are discussed. This is reason that MOFs as catalysts for electrochemical CO2RR offers several advantages over traditional catalysts, such as tunable surface structure, multifunctionality, selectivity control, and stability under CO2RR operation. And then, some of the most recent reported works on MOF‐based catalysts are summarized, to provide and inspire further investigations and ideas in this research field. However, despite these advantages, there are still research gaps that need to be addressed. Some of these gaps include being cost‐effective and economical process for preparing MOF‐based catalysts, long‐term stability for industrial usage, and scalability of the catalyst. Thereby, further studies are essential to fully exploit the potential of MOFs in advancing CO2RR technologies. [ABSTRACT FROM AUTHOR]

Metal–organic rotaxane compounds (MORCs) with supramolecular (pseudo)rotaxane motifs as main structures have inherent dynamic character, but their potential as responsive molecular machines is largely hampered by poor responsiveness to external stimuli. In this study, using a multi‐functionalized pseudorotaxane linker that combines two kinds of functionalities, a novel MORC, U‐bpybc‐CB8 (U refers to uranyl, bpybc refers to 1, 1'‐bis(4‐carboxybenzyl)‐4, 4'‐bipyridinium, and CB8 is cucurbit[8]uril), with multi‐responsive capability that can respond to both light and thermal stimuli, is reported. The characterization, combining spectra measurements and single‐crystal X‐ray diffraction, shows that, due to the involvement of viologen‐functionalized flexible organic dicarboxylate guest molecule in the CB8‐ involved pseudorotaxane ligand, the resultant uranyl‐based MORC exhibits photochromic behavior after UV or visible light irradiation. More interestingly, it is revealed that the exceptional thermal response of U‐bpybc‐CB8 as temperature increases from 170 to 270 K, i.e., volume expansion followed by contraction after the inflection temperature of ≈230 K, can be stemmed from the lattice flexibility of this metal–organic supramolecular network. The dual responsiveness of MORCs reported here demonstrates the potential of such supramolecular assemblies as smart molecular components like sensors and switches that respond to light irradiation or temperature changes. [ABSTRACT FROM AUTHOR]

Simple Summary: The identification of biological targets is an essential step in deciphering the mechanism of action of anticancer drugs. In this review, we chose to study the relationship between the inhibition of thioredoxin reductase (TrxR), a key enzyme in maintaining the redox balance of cells, and the cytotoxic effects of two groups of organometallic complexes. The first group is essentially composed of Au(I) and Au(III) complexes and the second one comprises metallocifens (organometallic complexes derived from tamoxifen). The results show that these two groups interact differently with TrxR at the molecular level. Even if the contribution of TrxR inhibition to the cytotoxicity of complexes is clearly established for many of them, the number of complexes for which TrxR inhibition plays a predominant role appears quite limited. Eventually, the antiproliferative activity of most of the complexes appears to stem from the interaction with several targets, a favorable strategy to tackle MDR tumors. Cancers classified as multidrug-resistant (MDR) are a family of diseases with poor prognosis despite access to increasingly sophisticated treatments. Several mechanisms explain these resistances involving both tumor cells and their microenvironment. It is now recognized that a multi-targeting approach offers a promising strategy to treat these MDR tumors. Inhibition of thioredoxin reductase (TrxR), a key enzyme in maintaining redox balance in cells, is a well-identified target for this approach. Auranofin was the first inorganic gold complex to be described as a powerful inhibitor of TrxR. In this review, we will first recall the main results obtained with this metallodrug. Then, we will focus on organometallic complexes reported as TrxR inhibitors. These include gold(I), gold(III) complexes and metallocifens, i.e., organometallic complexes of Fe and Os derived from tamoxifen. In these families of complexes, similarities and differences in the molecular mechanisms of TrxR inhibition will be highlighted. Finally, the possible relationship between TrxR inhibition and cytotoxicity will be discussed and put into perspective with their mode of action. [ABSTRACT FROM AUTHOR]

Alkaline phosphatase (ALP) is a phosphomonoester hydrolase and serves as a biomarker in various diseases. However, current detection methods for ALP rely on bulky instruments, extended time, and complex operations, which are particularly challenging in resource-limited regions. Herein, we synthesized a MOF-derived Fe-N-C nanozyme to create biosensors for the coulometric and visual detection of ALP. Specifically, we found the Fe-N-C nanozyme can efficiently oxidize 3,3′,5,5′-tetramethylbenzidine (TMB) to generate blue-colored tetramethyl benzidine (TMBox) without the need for H2O2. To construct the biosensor, we incorporated the ALP enzymatic catalytic reaction to inhibit the oxidation of TMB by Fe-N-C oxidase nanozyme. This biosensor showed rapid and highly sensitive detection of ALP in both buffer and clinical samples. The limit of detection (LOD) of our approach could be achieved at 3.38 U L−1, and the linear range was from 5 to 60 U L−1. Moreover, we also developed a visual detection for ALP by using a smartphone-based assay and facilitated practical and accessible point-and-care testing (POCT) in resource-limited areas. The visual detection method also achieved a similar LOD of 2.12 U L−1 and a linear range of 5–60 U L−1. Our approach presents potential applications for other biomarker detections by using ALP-based ELISA methods. [ABSTRACT FROM AUTHOR]

Low‐dimensional (low‐D) organic metal halide hybrids (OMHHs) have emerged as fascinating candidates for optoelectronics due to their integrated properties from both organic and inorganic components. However, for most of low‐D OMHHs, especially the zero‐D (0D) compounds, the inferior electronic coupling between organic ligands and inorganic metal halides prevents efficient charge transfer at the hybrid interfaces and thus limits their further tunability of optical and electronic properties. Here, using pressure to regulate the interfacial interactions, efficient charge transfer from organic ligands to metal halides is achieved, which leads to a near‐unity photoluminescence quantum yield (PLQY) at around 6.0 GPa in a 0D OMHH, [(C6H5)4P]2SbCl5. In situ experimental characterizations and theoretical simulations reveal that the pressure‐induced electronic coupling between the lone‐pair electrons of Sb3+ and the π electrons of benzene ring (lp‐π interaction) serves as an unexpected "bridge" for the charge transfer. Our work opens a versatile strategy for the new materials design by manipulating the lp‐π interactions in organic–inorganic hybrid systems. [ABSTRACT FROM AUTHOR]

Metallocenes are highly versatile organometallic compounds. The versatility of the metallocenes stems from their ability to stabilize a wide range of formal electron counts. To date, d-block metallocenes with an electron count of up to 20 have been synthesized and utilized in catalysis, sensing, and other fields. However, d-block metallocenes with more than formal 20-electron counts have remained elusive. The synthesis and isolation of such complexes are challenging because the metal–carbon bonds in d-block metallocenes become weaker with increasing deviation from the stable 18-electron configuration. Here, we report the synthesis, isolation, and characterization of a 21-electron cobaltocene derivative. This discovery is based on the ligand design that allows the coordination of an electron pair donor to a 19-electron cobaltocene derivative while maintaining the cobalt–carbon bonds, a previously unexplored synthetic approach. Furthermore, we elucidate the origin of the stability, redox chemistry, and spin state of the 21-electron complex. This study reveals a synthetic method, structure, chemical bonding, and properties of the 21-electron metallocene derivative that expands our conceptual understanding of d-block metallocene chemistry. We expect that this report will open up previously unexplored synthetic possibilities in d-block transition metal chemistry, including the fields of catalysis and materials chemistry. The synthesis and isolation of d-block metallocenes with more than 18-electron is challenging since metal–carbon bonds become weaker with increasing deviation from the 18-electron configuration. Here the authors report a formal 21-electron cobaltocene derivative by coordination of a two-electron donor to a 19-electron cobaltocene derivative while maintaining the cobalt-carbon bonds. [ABSTRACT FROM AUTHOR]

With the aim to combine more than one biologically‐active component in a single molecule, derivatives of ispinesib and its (S) analogue were prepared that featured ferrocenyl moieties or bulky organic substituents. Inspired by the strong kinesin spindle protein (KSP) inhibitory activity of ispinesib, the compounds were investigated for their antiproliferative activity. Among these compounds, several derivatives demonstrated significantly higher antiproliferative activity than ispinesib with nanomolar IC50 values against cell lines. Further evaluation indicated that the antiproliferative activity is not directly correlated with their KSP inhibitory activity while docking suggested that several of the derivatives may bind in a manner similar to ispinesib. In order to investigate the mode of action further, cell cycle analysis and reactive oxygen species formation were investigated. The improved antiproliferative activity of the most active compounds may be assigned to synergic effects of various factors such as KSP inhibitory activity due to the ispinesib core and ability to generate ROS and induce mitotic arrest. [ABSTRACT FROM AUTHOR]