Synthesis ,Characterization and invitro evaluation of anticancer activity of new hydroxamicacid basedHDACi containing substituted thaizolesas a cap linking moiety.

Fadil M. Hamed, M. .. Mohammad
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Abstract

The present study was undertaken to synthesize, characterize  and evaluate the anticancer activity of  new derivatives of hydroxamate –based HDACi  having S-subistituted-5-amino1,3,4thadiazole as a cap linking moiety ,with suitable aliphatic linker.The structures and purity of the targeted compounds were confirmed by TLC , FTIR ,H-NMR and mass spectroscopy and their anticancer activity were evaluated by comparative cytotoxic study , Using HeLa nuclear extract and normal embryonic fibroblasts cell lines.All the synthesized compounds shows good anticancer activity, represented by their high rate of growth inhibition on Hela cell line and low cytotocic effect on normal cell line .Compound (VAb) show the best safety index(SI) that represented by its  selective cytotoxic activity on HeLa cell linewith  low cytotoxic effect on normal embryonic cell line.
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含取代噻唑烷的新型羟酸基hdaci的合成、表征及体外抗癌活性评价。
本文合成了以5-氨基1,3,4噻二唑为连接基团,并配以合适的脂肪族连接剂的羟肟基HDACi新衍生物,对其抗癌活性进行了表征和评价。采用薄层色谱(TLC)、红外光谱(FTIR)、核磁共振(H-NMR)和质谱(mass spectrometry)等方法对目标化合物的结构和纯度进行了验证,并利用HeLa核提取物和正常胚胎成纤维细胞进行了细胞毒性对比研究。化合物(VAb)对Hela细胞株的选择性细胞毒活性最高,对正常胚胎细胞株的细胞毒作用最低,显示出良好的抗肿瘤活性。
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