Synthesis and cytotoxicity studies of novel [1,2,4] Triazolo [1,5-a]pyrimidine-7-amines

Article abstract of DOI:10.1248/cpb.56.941

A series of novel N-anilino-5-methyl-2-(3-(5-(alkylaminomethyl)furan-2-yl- methylthio)propyl)-[1,2,4]triazolo-[1,5-a]pyrimidine-7-amine derivatives were synthesized and evaluated for their in vitro cytotoxicity against two cancer cell lines, Bel-7402 and HT-1080. Compounds 9, 14, 19 and 23 possessed marked cytotoxicity, especially 23 (with IC₅₀ values of 15.0μM and 7.8μM against Bel-7402 and HT-1080 cell lines, respectively), which had emerged as lead compound. The activity was found to depend strongly on substitution pattern of the side chains at C-2 position, and 4-triflouromethylanilino substituent at C-7 position was an option for anticancer potency.