Synthesis, dihydrofolate reductase inhibition, anti-proliferative testing, and saturation transfer difference 1h-nmr study of some new 2-substituted-4, 6- …

…, E González, O Millet, JM Mato, F Kobarfard

Index: Mohebbi, Shohreh; Falcon-Perez, Juan Manuel; Gonzalez, Esperanza; Millet, Oscar; Mato, Jose Maria; Kobarfard, Farzad Chemical and Pharmaceutical Bulletin, 2012 , vol. 60, # 1 p. 70 - 78

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Citation Number: 8

Abstract

A series of 2-substituted-4, 6-diaminipyrimidine derivatives were synthesized and evaluated for their dihydrofolate reductase (DHFR) inhibitory activity. Saturation transfer difference (STD) 1 H-NMR experiments were used to probe the binding characteristics of the compounds with human DHFR enzyme. The most potent molecules, 12 and 15, in enzyme assay study showed the best results in STD experiments indicating their intimate ...