一类新型噻唑类和含噻唑基团的1,3,4-噻二唑类抗癌药物:合成、光谱研究、生物学评价及构效关系

Sobhi M. Gomha, N. A. Kheder, Mohamad R. Abdelaziz, Y. Mabkhot
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引用次数: 2

摘要

以2-(4-甲基-2-苯基噻唑-5-羰基)- n -苯肼碳硫酰胺为原料,与合适的肼酰氯反应,设计并制备了一系列新的噻唑基1,3,4-噻二唑类化合物。根据光谱证据和它们的替代合成确定了新合成化合物的结构。研究了13种新的1,3,4-噻二唑类化合物对肝癌细胞株HepG2的抗癌活性。并对它们的构效关系进行了研究。1,3,4-噻二唑12d、12c、6g、18b、6c和6f(IC50分别为0.82、0.91、1.06、1.25、1.29和1.88µM)对肝癌细胞株HepG2具有良好的抗肿瘤活性。
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A Novel Series of Thiazoles and 1,3,4-Thiadiazoles Bearing Thiazole Moiety as Anticancer Agents: Synthesis, Spectral Studies, Biological Evaluation and Structure Activity relationship
A novel series of thiazole based-1,3,4-thiadiazoles were designed and prepared via the reaction of the 2-(4-methyl-2-phenylthiazole-5-carbonyl)-N-phenylhydrazinecarbothioamide with the appropriate hydrazonoyl chlorides. The structures of the newly synthesized compounds were established based on spectroscopic evidences and their alternative syntheses. Thirteen new 1,3,4-thiadiazoles have been evaluated for their anticancer activity against liver carcinoma cell line (HepG2). Also, their structure activity relationship (SAR) was studied. The 1,3,4-thiadiazoles 12d, 12c, 6g,18b, 6c, and 6f(IC50 = 0.82, 0.91, 1.06, 1.25, 1.29 and 1.88 µM, respectively) have promising antitumor activity against liver carcinoma cell line (HepG2).
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