Synthesis and Anticancer Evaluation of Some Novel 5‐Amino[1,2,4]Triazole Derivatives

Abstract

Novel [1,2,4]triazole derivatives were synthesized via various synthetic pathways. Among which were different substituted [1,2,4]triazole analogues that were synthesized, in addition to various fused [1,2,4]triazolo[1,5‐ a ]pyrimidine derivatives, [1,2,4]triazolo[1,5‐ a ][1,3,5]triazines, and [1,2,4]triazolo[5,1‐ c ][1,2,4]triazines. Besides, benzo[h][1,2,4]triazolo[5,1‐ b ]quinazolines, [1,2,4]triazolo‐[5,1‐ b ]quinazoline, [1,2,4]triazolo[1,5‐ a ]quinazoline and [1,2,4]triazolo[5,1‐ d ][1,2,3,5]tetrazine derivatives were also synthesized. The newly synthesized compounds were evaluated for their in vitro anticancer activity against liver cancer HepG2 and breast cancer MCF7 cell lines compared with the reference drug doxorubicin. Compounds 4 , 7 , 15 , 17 , 28 , 34 , and 47 were found to exert promising anticancer activity against HepG2 cell line showing IC 50 values ranging from 17.69 to 25.4 μM/L, while compounds 7 , 14a , 17 , 28 , and 34 showed significant activity against MCF7 cell line with IC 50 values ranging from 17.69 to 27.09 μM/L.