New water-soluble duocarmycin derivatives: Synthesis and antitumor activity of A-ring pyrrole compounds bearing β-heteroarylacryloyl groups

N Amishiro, S Nagamura, E Kobayashi…

Index: Amishiro, Nobuyoshi; Nagamura, Satoru; Kobayashi, Eiji; Gomi, Katsushige; Saito, Hiromitsu Journal of Medicinal Chemistry, 1999 , vol. 42, # 4 p. 669 - 676

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Citation Number: 32

Abstract

A series of A-ring pyrrole compounds of duocarmycin bearing 4'-methoxy-β- heteroarylacryloyl groups were synthesized and evaluated for in vitro anticellular activity against HeLa S3 cells and in vivo antitumor activity against murine sarcoma 180 in mice. Most of the 4'-methoxy-β-heteroarylacrylates displayed in vitro anticellular activity equivalent to that of 4'-methoxycinnamates. Among the 8-O-[(N-methylpiperazinyl) carbonyl] ...