Intensely potent doxorubicin analogues: structure-activity relationship

D Farquhar, A Cherif, E Bakina…

Index: Farquhar, David; Cherif, Abdallah; Bakina, Elena; Arly Nelson Journal of Medicinal Chemistry, 1998 , vol. 41, # 6 p. 965 - 972

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Citation Number: 44

Abstract

N-(5, 5-Diacetoxypent-1-yl) doxorubicin (1b) is an intensely cytotoxic doxorubicin analogue that retains full potency against tumor cells that express elevated levels of P-glycoprotein and are resistant to doxorubicin. 1b was designed to be hydrolyzed in the presence of carboxylate esterases to N-(5-oxypent-1-yl) doxorubicin, an aldehyde capable of existing in equilibrium with a cyclic carbinolamine. To investigate the structural determinants of ...