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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…

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

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被引用次数: 109

摘要

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 ...

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