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Background: The lack of efficacious therapy for advanced melanoma and neuroblastoma makes new approaches necessary. Therefore, many scientists seek new, more effective, more selective and less toxic anticancer drugs. Objective: We propose the synthesis of the new functionalized analogs of 1-nitroacridine/4- nitroacridone connected to tuftsin/retro-tuftsin derivatives as potential anticancer agents. Methods: Acridine and acridone analogues were prepared by Ullmann condensation and then cyclization reaction. As a result of nucleophilic substitution reaction 1-nitro-9-phenoxyacridine or 1- chloro-4-nitro-9(10H)-acridone with the corresponding peptides, the planned acridine derivatives (10a-c, 12, 17-a-d, 19) have been obtained. The cytotoxic activity of the newly obtained analogs were evaluated against melanotic (Ma) and amelanotic (Ab) melanoma cell lines and neuroblastoma SH-SY5Y by using the XTT method. Apoptosis and cell cycle were analyzed by flow cytometry. Results: Among the investigated analogs compound 12 exhibited the highest potency comparable to dacarbazine action for amelanotic Ab melanoma cells. FLICA test (flurochrome-labeled inhibitors of caspases) showed that this analog significantly increased the content of cells with activated caspases (C+) among both neuroblastoma lines and only Ab melanoma line. Using phosphatidylserine (PS) externalization assay, 12 induced changes in the Ab melanoma plasma membrane structure as the externalization of phosphatidylserine (An+ cells). These changes in neuroblastoma cells were less pronounced. Conclusion: Analog 12 could be proposed as the new potential chemotherapeutic against amelanotic melanoma form especially.

N-substituted acridine-containing 1,2-dioxetanes have been recently proposed as thermochemiluminescence (TCL) universal labels for bioanalytical applications. The TCL properties of these compounds markedly depend on the nature of substituents of the acridine ring. In the attempt to obtain new TCL probes with improved properties and stability, the push-pull approach was adopted, in which both electron withdrawing and electron donating groups are present in the acridine moiety. The results have been useful to better understand the role of the different decorations at the acridine fluorophore in modulating the photophysical properties and the activation parameters of 1,2-dioxetane labels. Moreover, the great versatility and innovation of these molecules make them extremely attractive for bioanalytical applications, in particular as labels for immune- and gene-probe assays.

Exosomes are promising biomarkers for cancer screening, but the development of a robust approach that can sensitively and accurately detect exosomes remains challenging. In the present study, an aptasensor based on the multifunctional signal probe 10-benzyl-2-amino-acridone (BAA) was developed for the colorimetric and photoelectrochemical detection and quantitation of exosomes. Exosomes are captured by cholesterol DNA anchor-modified magnetic beads (MBs) through hydrophobic interactions. This capture process can be monitored under a confocal fluorescence microscope using BAA as the fluorescent signal probe. The aptamer modified copper oxide nanoparticles (CuO NPs) then bind to mucin 1 (MUC1) on the surface of the exosomes to form a sandwich structure (MBs-Exo-CuO NPs). Finally, the MBs-Exo-CuO NPs are dissolved in nitric acid to generate Cu2+, which inhibits the visible-light-induced oxidase mimic activity and photoelectrochemical activity of BAA simultaneously. The changes in absorbance and photocurrent intensities are directly proportional to the concentration of exosomes. In this dual-modal aptasensor, the colorimetric assay can achieve rapid screening and identification, which is especially useful for point-of-care testing. The UV–vis absorbance and photocurrent assays then provide quantitative information, with a limit of detection of 1.09 × 103 particles μL−1 and 1.38 × 103 particles μL−1, respectively. The proposed aptasensor thus performs dual-modal detection and quantitation of exosomes. This aptasensor provides a much-needed toolset for exploring the biological roles of exosomes in specific diseases, particularly in the clinical setting.

Organic room temperature phosphorescent (ORTP) compounds have recently emerged as a promising class of emissive materials with a multitude of potential applications. However, the number of building blocks that give rise to efficient ORTP materials is still limited, and the rules for engineering phosphorescent properties in organic solids are not well understood. Here, we report ORTP in a series of N-substituted acridone derivatives with electron-donating, electron-withdrawing, and sterically bulky substituents. X-ray crystallography shows that the solid-state packing varies progressively between coparallel and antiparallel π-stacking and separated π-dimers, depending on the size of the substituent. The detailed photophysical studies supported by DFT calculations reveal complex dynamics of singlet and triplet excited states, depending on the electronic effects of substituents and solid-state packing. The programmable molecular packing provides a lever to control the triplet-triplet annihilation that is manifested as delayed fluorescence in acridone derivatives with continuous (both parallel and antiparallel) π-stacking.

Nitric oxide (NO) is an important signaling molecule involved in a wide range of physiological and pathological processes. Fluorescent imaging is a useful tool for monitoring NO concentration, which could be essential in various biological and biochemical studies. Here, we report the design of a novel small-molecule fluorescent probe based on 9(10H)acridone moiety for nitric oxide sensing. 7,8-Diamino-4-carboxy-10-methyl-9(10H)acridone reacts with NO in aqueous media in the presence of O2, yielding a corresponding triazole derivative with fivefold increased fluorescence intensity. The probe was shown to be capable of nitric oxide sensing in living Jurkat cells.

Fluorescent amino acids are powerful biophysical tools as they can be used in structural or imaging studies of a given protein without significantly perturbing its native fold or function. Here, we have synthesized and characterized 7-(dimethylamino)acridon-2-ylalanine (Dad), a red-shifted derivative of the genetically-incorporable amino acid, acridon-2-ylalanine. Alkylation increases the quantum yield and fluorescence lifetime of Dad relative to a previously published amino acid, 7-aminoacridon-2-ylalanine (Aad). These properties of Dad make it a potentially valuable protein label, and we have performed initial testing of its ability to be genetically incorporated using an evolved aminoacyl tRNA synthetase., Graphical Abstract

A new coumarin-acridone fluorescent probe S was designed and synthesized, and the structure was confirmed with 1H/13C NMR spectrometry, single-crystal X-ray diffraction, and high-resolution mass spectrometry. This probe has high sensitivity and selectivity for Fe3+ over other testing metal ions at 420 or 436 nm in acetonitrile–MOPS (3-Morpholinopropanesulfonic Acid) buffer solution (20.0 μM, pH = 6.9, 8:2 (v/v)). Under physiological conditions, the probe displayed satisfying time stability with a detection limit of 1.77 µM. In addition, probe S was successfully used to detect intracellular iron changes through a fluorescence-off mode, and the imaging results of cells and zebrafish confirmed their low cytotoxicity and satisfactory cell membrane permeability, as well as their potential biological applications.

Evaluating the binding interaction between biomacromolecules and various chemical compounds is one of the most biologically researched topics. The present experimental study attempted to investigate the binding interaction between two types of acridone derivative, namely 8-chloro acridone (CA) and nitrile cyanide acridone (NCA) as antineoplastic agents and calf thymus DNA (ctDNA) by applying various spectroscopic techniques. The binding interactions were first characterized by fluorescence quenching experiments, and it was demonstrated that NCA had higher affinity to ctDNA and bound to it more tightly. Further analysis indicated that the quenching process between CA and ctDNA was controlled by a dynamic mechanism, while the dominant process in ctDNA–NCA interaction was static. Analysis of thermodynamic parameters showed that hydrophobic forces played a key role in the interaction between ctDNA and CA, whereas ctDNA–NCA complex was mainly stabilized by van der Waals interactions. In terms of the latter interaction, external binding also contributed to the stabilization of the formed complex. On the basis of RLS results, we concluded that CA had stronger potential toxicity on ctDNA than NCA. Fluorescence competition studies aimed at uncovering the mode of binding and indicated that CA and NCA probably intercalated into ctDNA. Thermal denaturation studies confirmed the displacement experiments and showed that CA brought about a stronger effect on the ctDNA stabilization. Data gathered by spectroscopy studies were further supported by viscosity experiments. These studies also showed that CA and NCA intercalated into ctDNA by a non-classical and classical mode, respectively. The results of circular dichroism experiments revealed no considerable conformational transition occurred in ctDNA upon the binding interactions and ctDNA remained in B-form. Based on the spectroscopic results and the binding affinity of CA to double-strand and single-strand ctDNA, we inferred that although CA predominantly intercalated into ctDNA, a small population of its molecules might bind to the grooves of ctDNA. In case of NCA, all the experimental results confirmed that NCA molecules intercalated into ctDNA by a classical mode.

A comprehensive spectroscopic, photophysical and electrochemical investigation of N-alkylacridones, their newly synthesised chlorosulfonyl and water-soluble sulfonic acid derivatives has been undertaken in solution at room temperature. The study includes absorption and emission spectra together with quantitative measurements of the deactivation of the first excited singlet state, from which the rate constants for all the decay processes has been obtained. A comparison on the gradual change of the electronic spectral and photophysical properties with the degree of substitution is considered. In addition the electrochemical behavior of the water-soluble acridones at different pH values was obtained by cyclic and differential pulse voltammetry. The oxidation mechanism of disulfonated acridone is found to occur in one consecutive and irreversible charge transfer pH-dependent reaction. The water-soluble acridones were found to display long lifetime values, dependent on the pH and solvent polarity. This opens a door for its use as selective probes for different cellular environment and targets.

In this article topical issues in treatment of acute respiratory infections in children and place of both exogenous interferons and interferon inducer drugs in their treatment are reviewed, including mechanisms of action, advantages and disadvantages of their application, special features of use in children. The latest clinical and laboratory data on the efficacy meglumine acridone acetate use in this pathology are given here. Depletion of inflammatory manifestations, correction of immune system imbalance were observed, leading to reduction of symptoms severity and disease duration, which, along with the good tolerability of the drug allows us to recommend it for widespread use in children.

The article justifies the use of interferon inducers in a clinical practice of pediatrician. The authors isolated a group of derivatives of acridone acetic acid, which effectiveness is associated with the features of pharmacokinetics and pharmacological activity. They demonstrated preventive and therapeutic efficacy of cycloferon in the complex treatment of children with influenza and other acute respiratory viral infections, herpes virus, arbovirus, rotavirus infections, viral hepatitis and tick-borne encephalitis due to its immunomodulatory potency. The article analyzed the use of cycloferon in frequently sick children, patients with allergic diseases, chronic tonsillitis, etc.; also it showed a decrease in the frequency of relapses of both infectious and allergic diseases, the possibility of combined use with other etiotropic and symptomatic drugs.

A class of π-extended BF2 β-diketone chromophores, ADBF2-a and ADBF2-b, that containing electron donating N-butyl acridone units have been synthesized. ADBF2-a and ADBF2-b are highly fluorescent with quantum efficiencies (ΦF) close to unity in toluene. The fluorescence of ADBF2-b displays more pronounced solvatochromism and shows a twisted intramolecular charge transfer (TICT) character in polar solvent and aggregation induced emission enhancement (AIEE) behavior. Furthermore, ADBF2-b shows high contrast and sensitive acid/base induced emission “On/Off” switching that result from the reversible protonation/deprotonation of the nitrogen atom. The compounds are also highly luminescent in solid state with a ΦF value of 0.63 for ADBF2-a and 0.28 for ADBF2-b. Single crystal analysis reveals the highly rigid and planar backbone of ADBF2-a. The emission stimuli-responsive properties of the compounds in solid state have been investigated. ADBF2-a shows yellow emission (λem = 564 nm) in crystalline state while turned to be orange (λem = 586 nm) after grinding. Intriguingly, CH2Cl2 vapor fuming of the ground solid led to red emissive (λem = 624 nm) solid, which turned to original yellow color with further CH2Cl2 vapor fuming. The solid of ADBF2-b emits red (λem = 645 nm) fluorescence in crystalline state and red-shifted to λem = 680 nm for amorphous solid after mechanical grinding. The crystalline state was recovered by CH2Cl2 vapor fuming. We believe that this BF2 system will inspire the development of high luminescent solid-state materials, and provide important insights into smart stimuli-responsive properties.

The weakly coordinating, ketone-directed, regioselective monoamidation of aromatic ketones, chalcone, carbazole, and benzophenones was achieved by employing high-valent cobalt and rhodium catalysis to access numerous biologically important molecular building blocks. This amidation proceeded smoothly with a variety of ketones and several amidating partners. The application of the products in the synthesis of various heterocycles, including acridones, indoles, quinoline, quinolones, quinolinones, and quinazolines, was also explored. The total synthesis of acridone-based alkaloids, namely, toddaliopsin A, toddaliopsin D, and arborinine, and the formal synthesis of acronycine and noracronycin were also accomplished by applying this method. A mechanistic study revealed this amidation reaction follows a base-assisted intermolecular electrophilic substitution pathway.

A novel fluorescence labeling reagent N-acetylhydrazine acridone (AHAD) was designed and synthesized. A highly sensitive high performance liquid chromatography (HPLC) method coupled with fluorescence detection to determine benzaldehyde after derivatization with AHAD was developed. Optimum derivatization was obtained at 40 °C for 30 min with trichloroacetic acid as catalyst. Benzaldehyde derivative was separated on a reversed-phase SB-C18 column in conjunction with a gradient elution and detected by fluorescence detection at excitation and emission wavelengths of 371 nm and 421 nm. The established method exhibited excellent linearity over the injected amount of benzaldehyde of 0.003 to 5 nmol mL−1. The method was successfully applied to the determination of serum semicarbazide-sensitive amine oxidase (SSAO) activity in humans. SSAO is a significant biomarker because serum SSAO activity is elevated in patients with Alzheimer's disease, vascular disorders, heart disease and diabetes mellitus. It was demonstrated that the SSAO activity of the hyperglycemic group (60 ± 4 nmol mL−1 h−1) was significantly higher than that of normal blood sugar group (44 ± 4 nmol mL−1 h−1) with P < 0.05.

Based on the molecular modelling studies, a rational modification of the lead molecule was made to develop highly potent compounds showing anti-cancer activity against human breast cancer cell lines MCF 7, MDA-MB-468 and T-47D. The most potent compounds have Log P and total polar surface area 4.4–5.4 and 59.8 A, respectively and they also exhibited promising ADME profile.

Acridine derivatives were first used as antibacterial and antiparasitic agents, later as antimalarial and anti-HIV drugs, and now as potentially anti-cancer agents due to their high cytotoxic activity. Due to their serious adverse effects, new synthetic derivatives were introduced and tested based on modified naturally occurring substances, such as acridone derivatives, which also exhibit potential anti-tumor activity. Most of them are DNA-damaging substances, causing relatively strong and selective destruction of tumor cells. We have tested in vitro anti-proliferative effects of newly-synthesized tetrahydroacrid derivatives, namely tacrine-coumarin hybrid molecules, on various human and mouse cancer cell lines. Our results showed that tacrine-coumarin hybrids with seven, eight, and nine methylene groups in spacer reduce proliferation of cancer cells. A hybrid with nine methylene groups had the most significant anti-cancer effect.

Donor–acceptor–donor materials (1,2) having acridone as acceptor unit and carbazole as donor were synthesized for optoelectronic applications. Carbazole was substituted on 2,7 positions of acridone in 1, while 3,6-trifluoromethylphenyl carbazole was substituted in 2. Steady-state and time-dependent emission properties of these compounds were studied in detail to get insight into their possible thermally activated delayed fluorescence (TADF) behavior. The singlet–triplet energy gap (ΔEST) was found to be as low as 0.17 eV (1) and 0.15 eV (2), favorable for TADF materials. Both these materials were found to be efficient green TADF emitters in organic light-emitting diode (OLED) devices. Interestingly, the TADF properties were observed for the first time in undoped 1,2-based devices, i.e., without host matrix, unlike the most commonly reported TADF emitters. Furthermore, an exciplex emission at 465 nm was observed in the blends of 1,2 with poly(vinylcarbazole) (PVK) in 1:7 (w/w) ratio. OLEDs with the blend o...

Self-assembled, porous coordination cages with a functional interior find application in controlled guest inclusion/release, drug delivery, separation processes, and catalysis. However, only few studies exist that describe their utilization for the development of self-assembled materials based on their 3-dimensional shape and external functionalization. Here, dodecyl chain-containing, acridone-based ligands (LA) and shape-complementary phenanthrene-derived ligands (LB) are shown to self-assemble to heteroleptic coordination cages cis-[Pd2(LA)2(LB)2]4+ acting as a gemini amphiphile (CGA-1; Cage-based Gemini Amphiphile-1). Owing to their anisotropic decoration with short polar and long nonpolar side chains, the cationic cages were found to assemble into vesicles with diameters larger than 100 nm in suitable polar solvents, visualized by cryo-TEM and Liquid-Cell Transmission Electron Microscopy (LC-TEM). LC-TEM reveals that these vesicles aggregate into chains and necklaces via long-range interactions. In addition, the cages show a rarely described ability to stabilize oil-in-oil emulsions.

WOS:000451818000007; This paper is devoted to study two acridone derivatives (A-2DPA and A-2PTz). These acridone compounds are synthesized and proposed as high performance visible light photoinitiators, in the presence of an iodonium salt or/and an amine (NPG or EDB), for both the free radical polymerization of (meth)acrylates and the cationic polymerization of epoxides upon irradiation with LED@405 nm. Excellent polymerization initiating abilities are found, and high final monomer conversions are obtained. A full picture of the involved photochemical mechanisms is provided. This paper is also concerned with the use of these acridone-based systems in new 3D printing resins. Finally, the usage of the new acridone derivatives for photopolyrners with low migration properties is particularly outlined.

Acridinium 9-carboxylic acid derivatives have been extensively used as chemiluminescent labels in diagnostic assays. Triggering acridinium with basic hydrogen peroxide produces a highly strained dioxetanone intermediate, which converts into an acridone in an electronically excited state and emits light at 420–440 nm. Here, we introduce a novel acridinium-fluorescein construct emitting at 530 nm, in which fluorescein is covalently attached to the acridinium N-10 nitrogen via a propyl sulfonamide linker. To characterize the spectral properties of the acridinium-fluorescein chemiluminophores, we synthesized the analogous acridone-fluorescein constructs. Both acridinium and acridone were linked to either 5- or 6-carboxyfluorescein and independently synthesized as individual structural isomers. Using fluorescent acridone-fluorophore tandems, we investigated and optimized the diluent composition to prevent dye aggregation. As monomolecular species, the acridone isomers demonstrated similar absorption, excitation, and emission spectra, as well as the expected fluorescence lifetimes and molecular brightness. Chemical triggering of acridinium-fluorescein tandems, as well as direct excitation of their acridone-fluorescein analogs, resulted in a nearly complete energy transfer from acridone to fluorescein. Acridone-based dyes can be studied with steady-state spectroscopy. Thus, they will serve as useful tools for structure and solvent optimizations, as well as for studying chemiluminescent energy transfer mechanisms in related acridinium-fluorophore tandems. Direct investigations of the light-emitting molecules generated in the acridinium chemiluminescent reaction empower further development of chemiluminescent labels with red-shifted emission. As illustrated by the two-color HIV model immunoassay, such labels can find immediate applications for multicolor detection in clinical diagnostic assays.

Drug resistance is one of the critical challenges faced in the treatment of Glioma. There are only limited drugs available in the treatment of Glioma and among them Temozolomide (TMZ) has shown some effectiveness in treating Glioma patients, however, the rate of recovery remains poor due to the inability of this drug to act on the drug resistant tumor sub-populations. Hence, in this study three novel Acridone derivative drugs AC2, AC7, and AC26 have been proposed. These molecules when combined with TMZ show major tumor cytotoxicity that is effective in suppressing growth of cancer cells in both drug sensitive and resistant sub-populations of a tumor. In this study a novel mathematical model has been developed to explore the various drug combinations that may be useful for the treatment of resistant Glioma and show that the combinations of TMZ and Acridone derivatives have a synergistic effect. Also, acute toxicity studies of all three acridone derivatives were carried out for 14 days and were found safe for oral administration of 400 mg/kg body weight on albino Wistar rats. Molecular Docking studies of acridone derivatives with P-glycoprotein (P-gp), multiple resistant protein (MRP), and O6-methylguanine-DNA methyltransferase (MGMT) revealed different binding affinities to the transporters contributing to drug resistance. It is observed that while the Acridone derivatives bind with these drug resistance causing proteins, the TMZ can produce its cytotoxicity at a much lower concentration leading to the synergistic effect. The in silico analysis corroborate well with our experimental findings using TMZ resistant (T-98) and drug sensitive (U-87) Glioma cell lines and we propose three novel drug combinations (TMZ with AC2, AC7, and AC26) and dosages that show high synergy, high selectivity and low collateral toxicity for the use in the treatment of drug resistant Glioma, which could be future drugs in the treatment of Glioblastoma.

The present article is a systematic and constructive review of the traditional medicinal uses, chemistry, pharmacology, toxicology, and formulation aspects of Glycosmis species. The genus Glycosmis comprise 51 accepted species broadly distributed in Australia, China, India, and South-East Asia. Traditionally, Glycosmis species are used in folk medicines to treat cancer, anaemia, rheumatism, fever, cough, liver-related problems, skin ailments, intestinal worm infections, wounds, and facial inflammation. This review aims to provide readers with the latest information highlighting chemical constituents isolated from the Glycosmis species, plant parts utilized for their isolation and their pharmacological activities. So far, 307 chemical constituents have been isolated and characterized from different species of the genus Glycosmis; among these constituents, alkaloids, flavonoids, terpenoids, phenolics, and sulphur-containing amides are the major bioactive compounds. Modern pharmacological studies have shown that the crude extracts and compounds isolated from this genus exhibit a broad spectrum of biological activities like anticancer, antimicrobial, anti-inflammatory, antipyretic, antidiabetic, antioxidant, larvicidal, insecticidal, hepatoprotective, wound healing, antiviral, antidiarrheal, and anxiolytic. The carbazole and acridone alkaloids from this genus have shown potential anticancer activity in various in vitro and in vivo studies. Rare scaffolds like dimeric carbazoles, dimeric acridone alkaloids, flavanocoumarins and sulphur-containing amides from this genus need further exploration for their potential bioactivity. This article also briefs about the toxicological screening and discusses various polyherbal and nano formulation aspects of Glycosmis species. Most of the pharmacological studies reported from this genus were carried out in vitro. An in-depth in vivo and toxicology evaluation of the crude extracts and isolated specialized compounds is required to explore the full therapeutic potential of this genus.

Inhibition of Yeast Topoisomerase II were analyzed according to relaxation assay kit from Inspiralis. Briefly, 250 ng of supercoiled pBR322 DNA, 1 mM ATP, 1-200 μM of analyzed compound were mixed with reaction buffer (1 mM Tris-HCl (pH 7.9), 10 mM KCl, 0.5 mM MgCl 2, 0.2 % (v/v) glycerol). The reaction was initiated by the addition of an enzyme, allowed to proceed at 30°C for 30 min and terminated by addition of 40% (w/v) sucrose, 100 mM Tris-HCl pH 8, 10 mM EDTA, 0.5 mg mL -1 Bromophenol Blue. Two step extraction with chloroform:isoamyl alcohol (24:1) and butanol water were made and mixtures were analyzed on the 1% agarose gel in 1x TAE buffer, 3h, 4.5 V cm -1. Gel was stained in GelRed 3x staining solution for 30 min and photographed with Gel Doc XR+Gel Documentation System.

The datasets contain the results of determining the minimum inhibitory concentration of imidazoacridinone derivatives against C. albicans ATCC 10231, C. glabrata ATCC 90030, C. krusei ATCC 6258 and C. parapsilosis ATCC 22019 and C. albicans clinical strains by the modified M27-A3 specified by the CLSI.

Optical measurements of C-1305 derivatives (IKE1-IKE8). The absorption spectra were recorded at 300 - 800 nm for solutions with 16 μg / mL derivative concentration. The fluorescence emission spectra were determined at 420-800 nm with the excitation wavelengths 360 or 415 nm for solutions with 1 μg / mL derivative concentration. All measurements were recorded using a multiplate reader Tecan Spark 10M.

International audience; Acridine- and acridone-based polycyclic aromatics were prepared by using as the key steps a copper-catalysed N-arylation of 2-aminobenzaldehyde, 2-aminophenones, or ethyl 2-aminobenzoate with 2-iodotriphenylene, and an acid-mediated cyclization. The regioselectivity of this intramolecular SEAr reaction was studied by performing Hückel theory calculations on the precursors. Due to their structural similarity with some MALDI-MS matrices, two acridine-based polycycles were evaluated for this purpose. Finally, in view of structure–property relationships, preliminary studies of the photophysical properties of the synthesized acridine- and acridone-based polycycles were performed.

Pt(IV) cored Gd(III) metal complex as a multimodal MRI contrast agent for cancer diagnosis is reported. The hetero nuclear complex [Pr-(DO3-Ch-Ph-Am-Gd(III))2Pt(II)] is highly soluble in water and stable at room temperature. The complex shows high longitudinal (r1p = 24.43 mM-1 s-1) and transversal (r2p = 38.61 mM-1 s-1) relaxivity values in neat aqueous solution at pH =7 and at 27 oC. The relaxivity value of the complex is greater than the low molecular weight, FDA approved MRI contrast agents. The presence of two water molecules in the first coordination sphere and a replaceable hydrogen atom in the linker enhances the proton relaxation rate and gives a huge relaxivity value. The r2p/r1P ratio of 1.58 confirms that the complex is a T1-weighted contrast agent. The presence of high polar coumarone pendant arm and high rigid acridone moieties in the complex make the complex as better anticancer agent for ovarian cancer. The high polar nature of the coumarone, phenyl amide, acridone moiety will show better binding efficiency with ovarian cancer creating CA125 glycoprotein.