Folate antagonists. 20. Synthesis and antitumor and antimalarial properties of trimetrexate and related 6-[(phenylamino) methyl]-2, 4-quinazolinediamines

EF Elslager, JL Johnson, LM Werbel

文献索引：Elslager, Edward F.; Johnson, Judith L.; Werbel, Leslie M. Journal of Medicinal Chemistry, 1983 , vol. 26, # 12 p. 1753 - 1760

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被引用次数: 81

摘要

A series of 6-[(arylamino) methyl]-2, 4-quinazolinediamines have been prepared by catalytic hydrogenation of the requisite 2, 4-diamino-6-quinazolinecarbonitriles in the presence of the appropriate benzenamine. Formylation, acetylation, and nitrosation provided N" derivatives of these compounds. A variety of the compounds exhibited potent antimalarial, antibacterial, and antitumor activity. In particular, 5-methyl-6-[[(3, 4, 5-trimethoxyphenyl)-amino] methyl]- ...