Search

Eosinophilic solid and cystic renal cell carcinoma (ESC-RCC) is a rare type of renal cell carcinoma with inert biological behavior that has not yet been included in the 2016 World Health Organization (WHO) classification, and its imaging manifestations are unclear due to its rarity. Although there have only been a few cases, the CT and MRI findings of ESC-RCC are characterized by its cystic solid structure, according to the proportion of cystic and solid components observed on images, ESC-RCC can be categorized into three types. Especially the Type I, when the cystic-solid components are almost equal, the imaging findings are illustrated as "lotus root-like," which may be helpful in the differential diagnosis of ESC-RCC from other types of renal tumors. In fact, ESC-RCC has diverse radiological appearances, and the differentiation of clear cell renal cell carcinoma, renal oncocytoma, chromophobe renal cell carcinoma, and renal angiomyolipoma remains challenging. This review aims to discuss ESC-RCC with a focus on the radiological findings and differential diagnosis of ESC-RCC. [ABSTRACT FROM AUTHOR]

A new narrowband thermally activated delayed fluorescence emitter, PhCzBN-PO, was developed by incorporating the diphenylphosphine oxide (DPPO) group into a multi-resonance core. The unique properties of DPPO enabled PhCzBN-PO to achieve pure green emission and a nonplanar structure. The resulting electroluminescent devices achieved high external quantum efficiencies up to 32.4% with extremely low efficiency roll-off and pure-green emission with Commission Internationale de L'Eclairage (CIE) coordinates of (0.24, 0.67). [ABSTRACT FROM AUTHOR]

[Display omitted] • Narrowband blue emitters are successfully achieved by decoration of multi-resonance emitter. • The decorating donor group was beneficial for accelerating the reverse intersystem crossing. • Blue organic light-emitting diodes with narrowband emission and high EQE up to 30.6% are achieved. Multi-resonance thermally activated delayed fluorescence (MR-TADF) emitters with high efficiency and narrowband blue emission are highly demanded for high-quality displays. In this study, two MR-TADF emitters, namely CzBN-tDPA and CzBN-mCP, were designed by decorating the well-known emitter of CzBN with different diarylamino moieties. This peripheral decoration strategy successfully results in blue emission with peaks at 465 and 464 nm, narrow full-width at half maximum (FWHM) values of 23 and 21 nm for CzBN-tDPA and CzBN-mCP in toluene solution, respectively. The new emitters exhibit faster rate constants of reverse intersystem crossing and higher photoluminescence quantum yields, compared to the parent molecule. As a result, organic light-emitting diodes based on CzBN-tDPA and CzBN-mCP exhibit narrowband blue emission with maximum external quantum efficiencies (EQE max s) of nearly 20% and low efficiency roll-offs. More importantly, decent EQE max up to 30.6% could be realized in hyperfluorescence devices adopting these two new emitters. [ABSTRACT FROM AUTHOR]

Reported herein is a chemical method for the direct resolution of unprotected racemic β-substituted-β-amino acids (β³-AAs) that uses specially designed, stable, and recyclable α- methylproline-derived chiral ligands. The versatility of this methodology is unmatched by biocatalytic approaches. The method shows a broad synthetic generality for various aryl- or alkyl-substituted β³-AAs, and the new nonracemizable ligands can be accessed readily. Furthermore, the presented method produces an excellent stereochemical outcome and has a fully recyclable source of chirality, and the reaction conditions are operationally simple and convenient. The procedure has also been successfully applied to the scalable synthesis of the anti- HIV drug maraviroc. [ABSTRACT FROM AUTHOR]

Approximately 20% of multiple myeloma (MM) are caused by a chromosomal translocation t (4; 14) that leads to the overexpression of the nuclear receptor binding SET domain-protein 2 (NSD2) histone methyltransferase. NSD2 catalyzes the methylation of lysine 36 on histone H3 (H3K36me2) and is associated with transcriptionally active regions. Using high-throughput screening (HTS) with biological analyses, a series of 5-aminonaphthalene derivatives were designed and synthesized as novel NSD2 inhibitors. Among all the prepared compounds, 9c displayed a good NSD2 inhibitory activity (IC 50 = 2.7 μM) and selectivity against both SET-domain-containing and non-SET-domain-containing methyltransferases. Preliminary research indicates the inhibition mechanism of compound 9c by significantly suppressed the methylation of H3K36me2. Compound 9c specifically inhibits the proliferation of the human B cell precursor leukemia cell line RS4:11 and the human myeloma cell line KMS11 by inducing cell cycle arrest and apoptosis with little cytotoxicity. It has been reported that the anti-cancer effect of compound 9c is partly achieved by completely suppressing the transcriptional activation of NSD2-targeted genes. When administered intraperitoneally at 25 mg/kg, compound 9c suppressed the tumor growth of RS4:11 xenografts in vivo and no body weight loss was detected in the tested SCID mice. [Display omitted] • 5-aminonaphthalene derivatives were designed, synthesized and evaluated, the SAR of these compounds was demonstrated. • Compound 9c exhibited a good NSD2 inhibitory activity and inhibited the proliferation of leukemia cell line. • The anti-cancer effect of 9c is partly achieved by suppressing the transcriptional activation of NSD2-targeted genes. • When administered intraperitoneally at 25 mg/kg, compound 9c suppressed the tumor growth of RS4:11 xenografts in vivo. [ABSTRACT FROM AUTHOR]

1,4‐BN‐doped polycyclic aromatic hydrocarbons (PAHs) have emerged as very promising emitters in organic light‐emitting diodes (OLEDs) due to their narrowband emission spectra that may find application in high‐definition displays. While considerable research has focused on investigating the properties of these materials, less attention has been placed on their synthetic methodology. Here we developed an efficient synthetic method for 1,4‐BN‐doped PAHs, which enables sustainable production of narrowband organic emitting materials. By strategically introducing substituents, such as methyl, tert‐butyl, phenyl, and chloride, at the C5 position of the 1,3‐benzenediamine substrates, we achieved remarkable regioselective borylation in the para‐position of the substituted moiety. This approach facilitated the synthesis of a diverse range of 1,4‐BN‐doped PAHs emitters with good yields and exceptional regioselectivity. The synthetic method demonstrated excellent scalability for large‐scale production and enabled late‐stage transformation of the borylated products. Mechanistic investigations provided valuable insights into the pivotal roles of electron effect and steric hindrance effect in achieving highly efficient regioselective borylation. Moreover, the outstanding device performance of the synthesized compounds 10 b and 6 z, underscores the practicality and significance of the developed method. [ABSTRACT FROM AUTHOR]

1,4‐BN‐doped polycyclic aromatic hydrocarbons (PAHs) have emerged as very promising emitters in organic light‐emitting diodes (OLEDs) due to their narrowband emission spectra that may find application in high‐definition displays. While considerable research has focused on investigating the properties of these materials, less attention has been placed on their synthetic methodology. Here we developed an efficient synthetic method for 1,4‐BN‐doped PAHs, which enables sustainable production of narrowband organic emitting materials. By strategically introducing substituents, such as methyl, tert‐butyl, phenyl, and chloride, at the C5 position of the 1,3‐benzenediamine substrates, we achieved remarkable regioselective borylation in the para‐position of the substituted moiety. This approach facilitated the synthesis of a diverse range of 1,4‐BN‐doped PAHs emitters with good yields and exceptional regioselectivity. The synthetic method demonstrated excellent scalability for large‐scale production and enabled late‐stage transformation of the borylated products. Mechanistic investigations provided valuable insights into the pivotal roles of electron effect and steric hindrance effect in achieving highly efficient regioselective borylation. Moreover, the outstanding device performance of the synthesized compounds 10 b and 6 z, underscores the practicality and significance of the developed method. [ABSTRACT FROM AUTHOR]

This review provides a brief assessment of the methodological field of trifluoromethylation and its possible impact on the development of new CF 3 -containing pharmaceuticals. Structural aspects of five new drug-candidates, [tafenoquine (aromatic CF 3 ), roniciclib (heteroaromatic CF 3 ), BAY-38-7271 (aliphatic CF 3 ), sonidegib (O CF 3 ) and navitoclax (S-CF 3 )] currently under the development in phase II and III clinical studies, and their biological properties, therapeutic area and synthesis are critically discussed. [ABSTRACT FROM AUTHOR]

Abstract: A series of biaryl-based chalcones were designed as a combination of the natural chalcone and biphenyl moieties, and synthesized by two step chemistry involving Knoevenagel reaction and microwave assistant Suzuki coupling. Sulforhodamine B (SRB) assay was performed to evaluate the cell viability inhibitory abilities of these compounds against five cancer cell lines (A549, CNE2, SW480, MCF-7, and HepG2) from different tissues. Their Nuclear Factor-κB (NF-κB) nuclear translocation inhibitory activities were further investigated by High Content Analysis (HCA) based assay. Most of the compounds showed moderate to strong anticancer and NF-κB nuclear translocation inhibition activities and potent compounds were found. [Copyright &y& Elsevier]

Microplastic contamination is ubiquitous in aquatic environments. As global plastic production increases, the abundance of microplastic contaminants released into the environment has also continued to soar. The hydrophobic surfaces of plastic particles can adsorb a variety of chemical pollutants, and could therefore facilitate toxin accumulation through the food chain. In this study, the adsorption behavior of aniline, a priority environmental pollutant from industrial production, on the surface of polystyrene microplastics (mPS) was investigated. The results showed that the maximum adsorption capacity of mPS was 0.060 mg/g. Adsorption equilibrium was reached after 24 h, and the pseudo-second-order model was employed to explain the adsorption kinetics of aniline on the mPS particles. The Freundlich models could describe the adsorption isotherms. The potential adsorption mechanisms may include π-π interactions and hydrophobic interactions. pH, ionic strength, and ambient temperature of the solution played important roles in the adsorption process. [Display omitted] • MPS showed significant adsorption potential to aniline. • The adsorption of aniline on mPS increased with the decrease of particle sizes. • π-π interactions and hydrophobic interactions were the main adsorption mechanisms. [ABSTRACT FROM AUTHOR]

Structurally simple and inexpensive chiral tridentate ligands were employed for substantially advancing the purely chemical dynamic kinetic resolution (DKR) of unprotected racemic tailor-made α-amino acids (TM-α-AAs), enabling the first DKR of TM-α-AAs bearing tertiary alkyl chains as well as multiple unprotected functional groups. Owing to the operationally convenient conditions, virtually complete stereoselectivity, and full recyclability of the source of chirality, this method should find wide applications for the preparation of TM-α-AAs, especially on large scale. [ABSTRACT FROM AUTHOR]

Structurally simple and inexpensive chiral tridentate ligands were employed for substantially advancing the purely chemical dynamic kinetic resolution (DKR) of unprotected racemic tailor-made α-amino acids (TM-α-AAs), enabling the first DKR of TM-α-AAs bearing tertiary alkyl chains as well as multiple unprotected functional groups. Owing to the operationally convenient conditions, virtually complete stereoselectivity, and full recyclability of the source of chirality, this method should find wide applications for the preparation of TM-α-AAs, especially on large scale. [ABSTRACT FROM AUTHOR]

Reported herein is the first purely chemical method for the dynamic kinetic resolution (DKR) of unprotected racemic α-amino acids (α-AAs), a method which can rival the economic efficiency of the enzymatic reactions. The DKR reaction principle can be readily applied for S/R interconversions of α-AAs, the methodological versatility of which is unmatched by biocatalytic approaches. The presented process features a virtually complete stereochemical outcome, fully recyclable source of chirality, and operationally simple and convenient reaction conditions, thus allowing its ready scalability. A quite unique and novel mode of the thermodynamic control over the stereochemical outcome, including an exciting interplay between axial, helical, and central elements of chirality is proposed. [ABSTRACT FROM AUTHOR]

Reported herein is the first purely chemical method for the dynamic kinetic resolution (DKR) of unprotected racemic α-amino acids (α-AAs), a method which can rival the economic efficiency of the enzymatic reactions. The DKR reaction principle can be readily applied for S/R interconversions of α-AAs, the methodological versatility of which is unmatched by biocatalytic approaches. The presented process features a virtually complete stereochemical outcome, fully recyclable source of chirality, and operationally simple and convenient reaction conditions, thus allowing its ready scalability. A quite unique and novel mode of the thermodynamic control over the stereochemical outcome, including an exciting interplay between axial, helical, and central elements of chirality is proposed. [ABSTRACT FROM AUTHOR]

A variety of biaryl-based chalcones are designed, synthesized and evaluated for their inhibitory activities against five cancer cell lines. [ABSTRACT FROM AUTHOR]

Abstract: A series of new 4-arylidene curcumin analogues (4-arylidene-1,7-bisarylhepta-1,6-diene-3,5-diones) were synthesized and found to be potent antiproliferative agents against a panel of cancer cell lines at submicromolar to low micromolar concentrations by SRB assay. Their inhibitory abilities against NF-κB was evaluated by High Content Analysis (HCA) based immunofluorescence assay; and the Akt signalling inhibition was determined by fluorescence polarization assay and western blot respectively. The Structure–Activity Relationship was discussed. Our results revealed that 4-arylidene curcumin analogues may work in a multi-targets manner in cancer cell. [Copyright &y& Elsevier]

A purely chemical approach for preparation of (R)-α-amino acids of growing biomedical and pharmaceutical importance is developed. [ABSTRACT FROM AUTHOR]

The purely chemical dynamic kinetic resolution of α‐amino acids bearing tertiary alkyl chains and multiple unprotected functional groups is based on the enantioselective formation of nickel(II) complexes and their disassembly under convenient conditions. In their Communication on page 12918 ff., H. Liu, V. A. Soloshonok et al. show that the specially designed chiral ligands can be easily recycled while the target amino acids are isolated in good yields and excellent enantioselectivities. [ABSTRACT FROM AUTHOR]

Die rein chemische dynamische kinetische Racematspaltung von α ‐ Aminosäuren mit tertiären Alkylketten und unterschiedlichsten funktionellen Gruppen basiert auf der enantioselektiven Bildung eines Nickel(II) ‐ Komplexes und dessen Hydrolyse. In der Zuschrift auf S. 13110 ff. zeigen H. Liu, V. A. Soloshonok et al., dass die hierfür entwickelten Liganden leicht wiederverwendet werden können, während die gewünschten Aminosäuren in guten Ausbeuten und mit exzellenter Enantioselektivität isoliert wurden. [ABSTRACT FROM AUTHOR]