Journal of medicinal chemistry

6-Substituted 2, 4-Diaminopyrido [3, 2-d] pyrimidine Analogues of Piritrexim as Inhibitors of Dihydrofolate Reductase from Rat Liver, Pneumocystis carinii, and …

A Gangjee, Y Zhu, SF Queener

文献索引：Gangjee, Aleem; Zhu, Yuanming; Queener, Sherry F. Journal of Medicinal Chemistry, 1998 , vol. 41, # 23 p. 4533 - 4541

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被引用次数: 42

摘要

The synthesis and biological activity are reported for 21 6-substituted 2, 4-diaminopyrido [3, 2-d] pyrimidine analogues (4-24) of piritrexim (PTX) as inhibitors of dihydrofolate reductase (DHFR) and as antitumor agents. Recombinant DHFR from Pneumocystis carinii (pc) and native DHFR from Toxoplasma gondii (tg) were the target enzymes tested; these organisms are responsible for fatal opportunistic infections in AIDS patients. Rat liver (rl) DHFR ...