DNA-directed alkylating agents. 3. Structure-activity relationships for acridine-linked aniline mustards: consequences of varying the length of the linker chain

…, TA Gourdie, TJ Boritzki, GL Gravatt…

Index: Valu, Kisione K.; Gourdie, Trudi A.; Boritzki, Theodore J.; Gravatt, G. Lance; Baguley, Bruce C.; et al. Journal of Medicinal Chemistry, 1990 , vol. 33, # 11 p. 3014 - 3019

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Citation Number: 58

Abstract

Four series of acridine-linked aniline mustards have been prepared and evaluated for in vitro cytotoxicity, in vivo antitumor activity, and DNA cross-linking ability. The anilines were attached to the DNA-intercalating acridine chromophores by link groups (-0-,-CH2-,-S-, and- SO2-) of widely varying electronic properties, providing four series of widely differing mustard reactivity where the alkyl chain linking the acridine and mustard moieties was ...