Synthesis and antitumor activity of novel 1-substituted 3-(4,5-substituted 1,2,4-triazol-3-yl)--carboline derivatives

Schiff bases, 1,2,4-triazolo[4,3- d ][1,2,3,4]thiatriazoles, and 1,2,4-triazolo[3,4- b ][1,3,4]thiadiazoles carrying the -carboline nucleus were synthesized from 3-(4-amino-5-mercapto-1,2,4-triazol-3-yl)--carbolines. The compounds were evaluated for their in vitro antitumor activity against eight human cancer cell lines. The 1,2,4-triazolo[4,3- d ][1,2,3,4]thiatriazole derivatives showed a broad spectrum of antitumor activity, with GI (50) values lower than 13 M for all cell lines tested. In general, all tested compounds showed potent activity against the breast (MCF-7) cancer cell line, with GI (50) values in the range of 2.07 to 4.58M512573577FAPESP – Fundação de Amparo à Pesquisa Do Estado De São PauloSem informaçã