合成、表征及含苯并噻唑基的硫脲衍生物的生物评价作为潜在的抗菌和抗癌药物。
Synthesis, characterization and biological evaluation of some thiourea derivatives bearing benzothiazole moiety as potential antimicrobial and anticancer agents.
机构信息
Department of Chemistry, Research Complex, Allama Iqbal Open University, Islamabad, Pakistan.
出版信息
Eur J Med Chem. 2010 Apr;45(4):1323-31. doi: 10.1016/j.ejmech.2009.12.016. Epub 2009 Dec 16.
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 IC(50) values were observed in the range of 18-26 microM and 38-46 microM, respectively.
五个系列的噻二唑衍生物带有苯并噻唑部分（20 个化合物）被有效地合成并评估了其抗菌和抗癌活性。结果表明，这些化合物对测试的微生物具有广谱的活性，并且对真菌的活性高于对细菌的活性。化合物 1b、2b、3b、4b 和 5b 表现出最大的抗菌活性。初步的构效关系研究表明，苯并噻唑环中的电子因素对这些化合物的抗菌活性有很大的影响。在初步的 MTT 细胞毒性研究中，发现这些硫脲衍生物（2d、5c 和 5d）最有效。在 MCF-7 和 HeLa 细胞中，IC(50)值分别在 18-26 μM 和 38-46 μM 的范围内。
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