Synthesis, characterization and biological evaluation of some thiourea derivatives bearing benzothiazole moiety as potential antimicrobial and anticancer agents
Synthesis, characterization and biological evaluation of some thiourea derivatives bearing benzothiazole moiety as potential antimicrobial and anticancer agents
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DOI：
10.1016/j.ejmech.2009.12.016
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发表时间：
2010-04-01
影响因子：
6.7
通讯作者：
Hussain, Rizwan
中科院分区：
文献类型：
--
作者：
Saeed, Sohail;Rashid, Naghmana;Hussain, Rizwan
合成了5个系列的含苯并噻唑基的硫脲衍生物（共20个化合物），并对其抑菌和抗癌活性进行了评价。结果表明，该类化合物对供试微生物具有广谱的抗菌活性，对真菌的抗菌活性高于细菌。化合物1b、2b、3b、4 b和5 b表现出最大的抗菌活性。构效关系的初步研究表明，苯并噻唑环上的电子因素对该类化合物的抑菌活性有很大影响。在初步的MTT细胞毒性研究中，硫脲衍生物（2d，5c和5d）被发现是最有效的。在MCF-7和HeLa细胞中，观察到IC 50值在18-26 μ M和38-46 μ M范围内。分别(C)2009年Elsevier Masson SAS。All rights reserved.
Five series of thiourea derivatives bearing benzothiazole moiety (20 compounds) were efficiently synthesized and evaluated for antimicrobial and anticancer activities. The results indicated that the compounds possessed a broad spectrum of activity against the tested microorganisms and showed higher activity against fungi than bacteria. Compounds 1b, 2b, 3b, 4b and 5b exhibited the greatest antimicrobial activity. Preliminary study of the structure activity relationship revealed that electronic factors in benzothiazole rings had a great effect on the antimicrobial activity of these compounds. In preliminary MTT cytotoxicity studies, the thiourea derivatives (2d, 5c and 5d) were found most potent. In MCF-7 and HeLa cells, the IC50 values were observed in the range of 18-26 mu M and 38-46 mu M. respectively. (C) 2009 Elsevier Masson SAS. All rights reserved.