Novel 8-deaza-5, 6, 7, 8-tetrahydroaminopterin derivatives as dihydrofolate inhibitor: Design, synthesis and antifolate activity

…, S Zhou, X Wang, Z Liu, L Zhang, J Cui, J Liu

Index: Zhang, Zhili; Wu, Jun; Ran, Fuxiang; Guo, Ying; Tian, Ran; Zhou, Shouxin; Wang, Xiaowei; Liu, Zhenming; Zhang, Liangren; Cui, Jingrong; Liu, Junyi European Journal of Medicinal Chemistry, 2009 , vol. 44, # 2 p. 764 - 771

Full Text: HTML

Citation Number: 12

Abstract

We report, for the first time, the synthesis and biological activities of 8-deaza-5, 6, 7, 8- tetrahydroaminopterin 9, and the 5-substituted and 5, 10-disubstituted analogues 11, 13, 15, and 17. The analogues were obtained from key compound diethyl 8-deaza-5, 6, 7, 8- tetrahydroaminopterin 8 following the catalytic reduction of the pyridine ring of diethyl 8- deaza aminopterin 5. The five novel 8-deaza-5, 6, 7, 8-tetrahydroaminopterin derivatives ...