3,5-双（吲哚基）-1,2,4-噻二唑的合成及其体外抗癌活性。
Synthesis and in-vitro anticancer activity of 3,5-bis(indolyl)-1,2,4-thiadiazoles.
机构信息
Department of Chemistry, Birla Institute of Technology and Science, Pilani 333 031, India.
出版信息
Bioorg Med Chem Lett. 2011 Oct 1;21(19):5897-900. doi: 10.1016/j.bmcl.2011.07.089. Epub 2011 Jul 30.
A series of 3,5-bis(indolyl)-1,2,4-thiadiazoles were synthesized and evaluated for their cytotoxicity against selected human cancer cell lines. The reaction of indole-3-thiocarboxamide 3 with iodobenzene diacetate underwent oxidative dimerization to give 3,5-bis(indolyl)-1,2,4-thiadiazoles 4a-n. Among the synthesized bis(indoly)-1,2,4-thiadiazoles, the compound 4h with 4-chlorobenzyl and methoxy substituents showed the most potent activity.
合成了一系列 3,5-双（吲哚基）-1,2,4-噻二唑，并评估了它们对选定的人类癌细胞系的细胞毒性。吲哚-3-硫代甲酰胺 3 与碘苯二乙酸反应经历氧化二聚化生成 3,5-双（吲哚基）-1,2,4-噻二唑 4a-n。在所合成的双（吲哚基）-1,2,4-噻二唑中，带有 4-氯苄基和甲氧基取代基的化合物 4h 显示出最强的活性。
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