Synthesis, structural characterization and antitumor activity of novel 2,4-diamino-1,3,5-triazine derivatives

The syntheses, structural elucidation based on NMR spectroscopy and X-ray a nalysis of 8 as well as antitumor activities of novel 2,4-diamino-1,3,5-tri azine derivatives 5 and 7-22 are described. Screenings performed at NCI sho wed that most derivatives possessed a moderate to strong growth inhibition activity on various tumor panel cell lines between 0.148 and 56.2 muM conce ntrations. 2-Amino-6-bromomethy1-4-(3,5,5-trimethyl-2-pyrazoline)-1,3,5-tri azine 11 showed the most potent antitumor activity with the mean midpoint v alues of log(10) GI50. log(10) TGI50 and log,, LC50 of all tests equal to - 5.26, - 4.81 and - 4.37. respectively and therefore, it can be considered as a lead structure for further development of anticancer agents. (C) 2000 Editions scientifiques et medicales Elsevier SAS.