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含 1,3-硒唑基的 1,3,4-噻二唑衍生物的合成与抗肿瘤活性评价。

Synthesis and antitumor-evaluation of 1,3-selenazole-containing 1,3,4-thiadiazole derivatives.

机构信息

Department of Chemistry and Chemical Engineering, Tianjin University of Technology, Tianjin 300384, PR China.

出版信息

Bioorg Med Chem Lett. 2013 Dec 15;23(24):6577-9. doi: 10.1016/j.bmcl.2013.10.062. Epub 2013 Nov 6.

Abstract

A series of novel 1,3-selenazole-containing 1,3,4-thiadiazole derivatives bearing Schiff base moieties were synthesized and evaluated for their in vitro antiproliferative activities against human breast cancer cell MCF-7 and mouse lymphocyte leukemia cell L1210 by CCK-8 assay. The majority of the compounds showed better activity against MCF-7 cell, compared with lead compound PCS. In particular, compound 6c was the most potent compound with IC50 value of 4.02 μM.

摘要

一系列新型含 1,3-硒唑的 1,3,4-噻二唑衍生物带有席夫碱部分,通过 CCK-8 法评估了它们对人乳腺癌细胞 MCF-7 和小鼠淋巴细胞白血病细胞 L1210 的体外增殖活性。与先导化合物 PCS 相比,大多数化合物对 MCF-7 细胞表现出更好的活性。特别是,化合物 6c 是最有效的化合物,IC50 值为 4.02 μM。

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