Synthesis and evaluation of DNA-targeted spatially separated bis (aniline mustards) as potential alkylating agents with enhanced DNA cross-linking capability

…, AS Prakash, LPG Wakelin, PD Woodgate…

Index: Gourdie; Prakash; Wakelin; Woodgate; Denny Journal of Medicinal Chemistry, 1991 , vol. 34, # 1 p. 240 - 248

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Citation Number: 32

Abstract

DNA-targeted separated bis-mustards were synthesized by attaching aniline mono- mustards at the 4-and 9-positions of the DNA-intercalating ligand 9-aminoacridine-4- carboxamide, with the intention of improving the low cross-link to monoadduct ratio found with most alkylating agents. The geometry of these compounds requires that, when the acridine binds to DNA by intercalation, one alkylating moiety is delivered to each DNA ...