Synthesis of water-soluble (aminoalkyl) camptothecin analogs: inhibition of topoisomerase I and antitumor activity

…, LF Faucette, RK Johnson, RP Hertzberg

Index: Kingsburgy; Boehm; Jakas; Holden; Hecht; Gallagher; Caranfa; McCabe; Faucette; Johnson; Hertzberg Journal of Medicinal Chemistry, 1991 , vol. 34, # 1 p. 98 - 107

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Citation Number: 581

Abstract

Water-soluble analogues of the antitumor alkaloid camptothecin (1) were prepared in which aminoakyl groups were introduced into ring A or B. Most of the analogues were prepared by oxidation of camptothecin to 10-hydroxycamptothecin (2) followed by a Mannich reaction to give N-substituted g-(aminomethyl)-10-hydroxycamptothecins (4-12) or by subsequent modification of Mannich product 4 (13, 15, 17, 19, 21). Others were obtained by ...