Synthesis and biological activity of 3-and 5-amino derivatives of pyridine-2-carboxaldehyde thiosemicarbazone

…, TS Lin, JG Cory, AH Cory, AC Sartorelli

Index: Liu, Mao-Chin; Lin, Tai-Shun; Cory, Joseph G.; Cory, Ann H.; Sartorelli, Alan C. Journal of Medicinal Chemistry, 1996 , vol. 39, # 13 p. 2586 - 2593

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Citation Number: 71

Abstract

A series of 3-and 5-alkylamino derivatives, as well as other structurally modified analogues of pyridine-2-carboxaldehyde thiosemicarbazone, have been synthesized and evaluated as inhibitors of CDP reductase activity and for their cytotoxicity in vitro and antineoplastic activity in vivo against the L1210 leukemia. Alkylation of 3-and 5-amino-2-(1, 3-dioxolan-2- yl) pyridines (1, 2) resulted in corresponding 3-methylamino, 5-methylamino, 3-allylamino, ...