Synthesis and anti-cancer screening of novel heterocyclic-(2H)-1,2,3-triazoles as potential anti-cancer agents

trans -Cyanocombretastatin A-4 ( trans -CA-4) analogues have been structurally modified to afford their more stable CA-4-(2 H )-1,2,3-triazole analogues. Fifteen novel, stable 4-heteroaryl-5-aryl-(2 H )-1,2,3-triazole CA-4 analogues ( 8a-i , 9 and 11a-e ) were evaluated for anti-cancer activity against a panel of 60 human cancer cell lines. These analogues displayed potent cytotoxic activity against both hematological and solid tumor cell lines with GI 50 values in the low nanomolar range. The most potent compound, 8a , was a benzothiophen-2-yl analogue that incorporated a 3,4,5-trimethoxyphenyl moiety connected to the (2 H )-1,2,3-triazole ring system. Compound 8a exhibited GI 50 values of