European Journal of Medicinal Chemistry p. 1053 - 1064 (2000)
Update date:2022-09-26
Topics:
Brzozowski
Saczewski
Gdaniec
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.
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