2, 4-Diamino-5-chloroquinazoline analogs of trimetrexate and piritrexim: synthesis and antifolate activity

A Rosowsky, CE Mota, JE Wright…

文献索引：Rosowsky; Mota; Wright; Queener Journal of Medicinal Chemistry, 1994 , vol. 37, # 26 p. 4522 - 4528

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被引用次数: 45

摘要

Ten heretofore undescribed 2, 4-diamino-5-chloroquinazoline analogues of trimetrexate (TMQ) and piritrexim (PTX) were synthesized and tested as inhibitors of dihydrofolate reductase (DHFR) from rat liver, Pneumocystis carinii, and Toxoplasma gondii. The most active quinazolines against both the P. carinii and the T. gondii enzyme were those with an ArCH2-NH or ArNHCHz side chain. Among ArNH (CH21, compounds with n= 1-3 and ...