Antitumor properties of 2 (1H)-pyrimidinone riboside (zebularine) and its fluorinated analogs

JS Driscoll, VE Marquez, J Plowman…

Index: Driscoll, John S.; Marquez, Victor E.; Plowman, Jacqueline; Liu, Paul S.; Kelley, James A.; Barchi, Joseph J. Journal of Medicinal Chemistry, 1991 , vol. 34, # 11 p. 3280 - 3284

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Citation Number: 68

Abstract

2 (Yi)-F'yrimidinone riboside (zebularine, lb) and its Bfluoro (6b) and 2'-am-fluoro (7b) analogua have been synthesized and evaluated in vivo as antitumor agents. Zebularine provides increase in life span (ILS) values of ca. 70% against intraperitoneal (ip) murine B16 melanoma and 50% against P388 leukemia. This compound is active when administered either ip or orally against ip or subcutaneously implanted L1210 leukemia, producing ILS ...