Synthesis of some 3,5-diphenyl-4H-l,2,4-triazole derivatives as antitumor agents

摘要

A series of 4-arylidenamino-4H-1,2,4-triazoles 2-14 and 4-(l-aryl)cthylidcnamino-4H-1,2,4-triazolcs 28-30 have been synthesized by the treatment of 4-amino-4H-1,2,4-triazole 1 with certain aldehydes and ketones.Compounds 2-14 and 28-30 have been reduced with NaBH_4 to afford the corresponding 4-arylmethylamino-4H-1,2,4-triazolcs 15-27 and 4-(l-aryl)cthylamino-4H-l,2,4-triazoles 31-33.The compounds 2-33 have been characterized by ~1H NMR,~(13)C NMR,IR,Mass and UV-Vis spectral data.Compounds 12,17,18,19,20,21,22,24,29 and 32 have been screened on three human tumor cell lines,breast cancer (MCF7),non small cell lung cancer (NCI-H460),and CNS cancer (SF-268) at the National Cancer Institute (NIH),USA.The compounds are found to exhibit low antiprolifcrative activity in the anticancer tests.