Indolequinone antitumor agents: reductive activation and elimination from (5-methoxy-1-methyl-4, 7-dioxoindol-3-yl) methyl derivatives and hypoxia-selective …

…, E Swann, SA Everett, M Jaffar, J Nolan…

Index: Naylor, Matthew A.; Swann, Elizabeth; Everett, Steven A.; Jaffar, Mohammed; Nolan, John; Robertson, Naomi; Lockyer, Stacey D.; Patel, Kantilal B.; Dennis, Madeleine F.; Stratford, Michael R. L.; Wardman, Peter; Adams, Gerald E.; Moody, Christopher J.; Stratford, Ian J. Journal of Medicinal Chemistry, 1998 , vol. 41, # 15 p. 2720 - 2731

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Citation Number: 72

Abstract

A series of indolequinones bearing a variety of leaving groups at the (indol-3-yl) methyl position was synthesized by functionalization of the corresponding 3-(hydroxymethyl) indolequinone, and the resulting compounds were evaluated in vitro as bioreductively activated cytotoxins. The elimination of a range of functional groups carboxylate, phenol, and thiol was demonstrated upon reductive activation under both chemical and ...