Synthesis and biological evaluation of 1,2,4-triazole and 1,3,4-thiadiazole derivatives as potential cytotoxic agents.
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.
State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University.
Yao-Jie
YJ
Shi
Xue-Jiao
XJ
Song
Xiao
X
Li
Ting-Hong
TH
Ye
Ying
Y
Xiong
Luo-Ting
LT
Yu
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004261:DNA Replication / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D045325:HCT116 Cells; D006801:Humans; D013329:Structure-Activity Relationship; D013830:Thiadiazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity*; D014230:Triazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity*
D000970:Antineoplastic Agents; D013830:Thiadiazoles; D014230:Triazoles; C058949:1,3,4-thiadiazole; C045575:1,2,4-triazole