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

Article abstract of DOI:10.1016/S0223-5234(00)01194-6

The syntheses, structural elucidation based on NMR spectroscopy and X-ray analysis of 8 as well as antitumor activities of novel 2,4-diamino-1,3,5-triazine derivatives 5 and 7-22 are described. Screenings performed at NCI showed that most derivatives possessed a moderate to strong growth inhibition activity on various tumor panel cell lines between 0.148 and 56.2 μM concentrations. 2-Amino-6-bromomethyl-4-(3,5,5-trimethyl-2-pyrazoline)-l,3,5-triazine 11 showed the most potent antitumor activity with the mean midpoint values of log₁₀ GI50, log₁₀ TGI50 and log₁₀ 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.