Aim: To evaluate the cytotoxic activity of newly synthesized a series of novel HDAC inhibitors comprising sulfonamide as zinc binding group and Isatin derivatives as cap group joined by mono amide linker as required to act as HDAC inhibitors. Materials and Methods: The utilization of sulfonamide as zinc binding group joined by N-alkylation reaction with ethyl-bromo hexanoate as linker group that joined by amide reaction with Isatin derivatives as cap groups which known to possess antitumor activity in the designed of new histone deacetylase inhibitors and using the docking and MTT assay to evaluate the compounds. Results: Four compounds have been synthesized and characterized successfully by ART-FTIR, NMR and ESI-Ms. the compounds were synthesized and characterized by successfully by ART-FTIR, NMR and ESI- Ms. Assessed for their cytotoxic activity against human colon adenocarcinoma MCF-7 (IC50, I=105.15, II=60.00, III=54.11, IV=56.57, vorinostat=28.41) and hepatoblastoma HepG2 (IC50, I=63.91, II=135.18, III=118.85, IV=51.46, vorinostat=37.50). Most of them exhibited potent HDAC inhibitory activity and significant cytotoxicity. Conclusions: The synthesized compounds (I, II, III and IV) showed cytotoxicity toward MCF-7 and HepG2 cancer cell lines and their docking analysis provided a preliminary indication that they are viable [HDAC6] candidates.
حضرت معقدات كل من الفنادايل, الخارصين, النحاس والكادميوم بتكافؤهم الثنائي والذهب بتكافؤه الثلاثي بأستخدام صبغة ازوجديدة (6،4،2-ثلاثي هيدروكسي-3-((3-هيدروكسي فنيل) ثنائي زينيل ) فنيل ) ايثان-1-اون المحضرة من ملح الديازونيوم مع ٦,٤,٢- ثلاثي هيدروكسي اسيتوفينون بعد عزل (E)-1-(2,4,6-trihydroxy-3-((3-hydroxyphenyl)diazenyl)phenyl)ethan-1-one تم تشخيصها بواسطة الطرق الطيفية المتاحة والتقنيات التشخيصية لكل من التحليل الدقيق للعناصرواطياف كل من ال
... Show MoreIn this research various of 2,5-disubstituted 1,3,4-oxadiazole (Schiff base, oxo-thiazolidine , and other compounds) were synthesized from 2,5-di(4,4?- amino-1,3,4-oxadiazole ) which use quently synthesized from mixture of 4-amino benzoic acid and hydrazine in the presence of polyphosphorus acid. The synthesized compounds were characterized by using some Spectral data (UV, FT-IR, and 1H-NMR).
Objective: Synthesis, Characterization of formazan derivatives and studies the antioxidant activity of prepared compounds and molecular docking. Methods: In this study, formazan compounds (III–XIV) were produced by combining Schiff base compounds (I), (II) with diazonium salts resulting from reactions of different aromatic amines with sodium nitrate in the presence of Con.HCl at 0–5°C. When isonicotinic acid hydrazide reacts with (N,N-dimethylbenzaldehyde, 4-hydroxy-3-methoxybenzaldehyde) in the presence glacial acetic acid as a solvent Schiff base compounds are created. Results: The prepared compounds were identified by FT-IR, 1H NMR, 13C NMR, then the antioxidant activity of the derivatives and molecular docking were studied. D
... Show MoreA new carbonyl complexes of triazole and oxadiazole were synthesized. These complexes were identified and their structural geometric were suggested by using FT-IR and UV-Vis spectra, conductivity measurements and other chemical and physical properties. The spectra data (FT-IR, UV, Vis.) with the substantial aid of group theoretical calculations gave so many evidences for the proposed geometries and the type of bonding of these compounds
Abstract As a part of our ongoing project on the design and synthesis of new 4-thiazolidinone derivatives with antimicrobial activity, four new 4-thiazolidinone derivatives carrying bromo, nitro, methyl, and chloro groups on the benzene ring were synthesized by starting with the 7-amino-4-methylcoumarin moiety, linking coumarin with various phenyl isothiocynate to form the thiourea group, and then cyclizing the derivatives, characterized by IR and 1HNMR, and assayed in vitro for their antimicrobial activity against Gram positive and Gram negative bacteria and fungi. Overall, 2-(4-methyl-2-oxo-2H-chromen-3-yl)-3-(4-nitrophenyl) thiazolidin-4-one to be the most powerful individuals in the series. Based on the observed data, it can be sta
... Show MoreNew Schiff-base ligands bearing tetrazole moiety and their polymeric metal complexes with Co(II), Ni(II) and Cd(II) ions are reported. Ligands were prepared in a multiple-step reaction. The reaction of sodium 2,6- diformylphenolate and cyclohexane-1,3-dione with 5-amino-2-fluorobenzonitrile resulted in the isolation of two precursors sodium 2,6-bis((E)-(3-cyano-4-fluorophenylimino)methyl)-4-methylphenolate 1 and 5,5'- (1E,1'E)-cyclohexane-1,3-diylidenebis- (azan-1-yl-1-ylidene)bis(2-fluorobenzonitrile) 2, respectively. The reaction of precursors with azide gave the required ligands; sodium 2,6-bis((E)-(4-fluoro-3-(1H-tetrazol-5- yl)phenylimino)methyl)-4-methylphenolate (NaL) and (N,N'E,N,N'E)-N,N'-(cyclohexane-1,3-diylidene)bis(4- fluoro-3-
... Show MoreNew Schiff-base ligands bearing tetrazole moiety and their polymeric metal complexes with Co(II), Ni(II) and Cd(II) ions are reported. Ligands were prepared in a multiple-step reaction. The reaction of sodium 2,6- diformylphenolate and cyclohexane-1,3-dione with 5-amino-2-fluorobenzonitrile resulted in the isolation of two precursors sodium 2,6-bis((E)-(3-cyano-4-fluorophenylimino)methyl)-4-methylphenolate 1 and 5,5'- (1E,1'E)-cyclohexane-1,3-diylidenebis- (azan-1-yl-1-ylidene)bis(2-fluorobenzonitrile) 2, respectively. The reaction of precursors with azide gave the required ligands; sodium 2,6-bis((E)-(4-fluoro-3-(1H-tetrazol-5- yl)phenylimino)methyl)-4-methylphenolate (NaL) and (N, N'E, N, N'E)-N, N'-(cyclohexane-1,3-diylidene)bis(4- fluor
... Show MoreDerivatives of Schiff-bases possess a great importance in pharmaceutical chemistry. They can be used for synthesizing different types of bioactive compounds. In this paper, derivatives of new Schiff bases have been synthesized from several serial steps. The acid (I) was synthesized from the reaction of dichloroethanoic acid with 2 moles of p-aminoacetanilide. New acid (I) converted to its ester (II) via the reaction of (I) with dimethyl sulphate in the present of anhydrous of sodium carbonate and dry acetone. Acid hydrazide (III) has been synthesized by adding 80% of hydrazine hydrate to the new ester using ethanol as a solvent. The last step included the preparation of new Schiff-bases (IV-VIII) by the reaction of acid hydrazide with app
... Show MoreDerivatives of Schiff-bases possess a great importance in pharmaceutical chemistry. They can be used for synthesizing different types of bioactive compounds. In this paper, derivatives of new Schiff bases have been synthesized from several serial steps. The acid (I) was synthesized from the reaction of dichloroethanoic acid with 2 moles of p-aminoacetanilide. New acid (I) converted to its ester (II) via the reaction of (I) with dimethyl sulphate in the present of anhydrous of sodium carbonate and dry acetone. Acid hydrazide (III) has been synthesized by adding 80% of hydrazine hydrate to the new ester using ethanol as a solvent. The last step included the preparation of new Schiff-bases (IV-VIII) by the reaction of acid hydrazide with
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