Non-classical antifolates, 5-(N-phenylpyrrolidin-3-yl)-2, 4, 6-triaminopyrimidines and 2, 4-Diamino-6 (5H)-oxopyrimidines, synthesis and antitumor studies

…, TC Chao, VA Bacherikov, KT Chen, CM Chen…

Index: Huang, Yen-Lin; Lin, Chyun-Feng; Lee, Yi-Jen; Li, Wei-Wei; Chao, Ting-Chou; Bacherikov, Valeriy A.; Chen, Kuo-Tung; Chen, Chin-Ming; Su, Tsann-Long Bioorganic and Medicinal Chemistry, 2003 , vol. 11, # 1 p. 145 - 157

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Citation Number: 17

Abstract

A series of non-classical antifolates, namely 5-(N-phenylpyrrolidin-3-yl)-2, 4, 6- triaminopyrimidines (25a–i) and 2, 4-diamino-(N-phenylpyrrolidin-3-yl)-6 (5H)- oxopyrimidines (26a, b, c, f, h, i) was synthesized and evaluated for their in vitro cytotoxicity. Reacting aniline derivatives with 1, 4-dibromo-2-butanol gave 1-phenyl-3-pyrrolidinols (19a-– i), which were oxidized to pyrrolidin-3-ones (20a–i). The Knoevenagel reaction of 20a–i ...