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Synthesis and biological evaluation of 1,2,4-triazole and 1,3,4-thiadiazole derivatives as potential cytotoxic agents.

作者信息

Shi Yao-Jie, Song Xue-Jiao, Li Xiao, Ye Ting-Hong, Xiong Ying, Yu Luo-Ting

机构信息

State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University.

出版信息

Chem Pharm Bull (Tokyo). 2013;61(11):1099-104. doi: 10.1248/cpb.c13-00242. Epub 2013 Aug 10.

DOI:10.1248/cpb.c13-00242
PMID:23934258
Abstract

A series of new 3-amino-5-sulfanyl-1,2,4-triazole and 2-amino-5-sulfanyl-1,3,4-thiadiazole derivatives have been synthesized and their cytotoxicities were evaluated on a panel of human cancer cell lines (BxPC-3, H1975, SKOV-3, A875, HCT116, etc.). The best one (compound 5m) exhibited activities with IC50 values ranging from 0.04 to 23.6 µM against nine human cancer cell lines. Further biological evaluation indicated that DNA replication was blocked by treatment with compound 5m in HCT116 cells.

摘要

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