DNA-directed alkylating agents. 1. Structure-activity relationships for acridine-linked aniline mustards: consequences of varying the reactivity of the mustard

…, LPG Wakelin, WR Wilson, PD Woodgate…

Index: Gourdie; Valu; Gravatt; Boritzki; Baguley; Wakelin; Wilson; Woodgate; Denny Journal of Medicinal Chemistry, 1990 , vol. 33, # 4 p. 1177 - 1186

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Citation Number: 109

Abstract

A series of DNA-targeted aniline mustards have been prepared, and their chemical reactivity and in vitro and in vivo cytotoxicity have been evaluated and compared with that of the corresponding simple aniline mustards. The alkylating groups were anchored to the DNA- intercalating 9-aminoacridine chromophore by an alkyl chain of fixed length attached at the mustard 4-position through a link group X, while the corresponding simple mustards ...