DNA-directed alkylating agents. 4. 4-anilinoquinoline-based minor groove directed aniline mustards

GL Gravatt, BC Baguley, WR Wilson…

Index: Gravatt, G. Lance; Baguley, Bruce C.; Wilson, William R.; Denny, William A. Journal of Medicinal Chemistry, 1991 , vol. 34, # 5 p. 1552 - 1560

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Citation Number: 35

Abstract

A series of 4-anilinoquinoline-linked aniline mustards of widely varying mustard reactivity were prepared and evaluated for their antitumor activity. The compounds were designed as minor groove binding agents, where the aniline mustard ring is itself part of the DNA-binding ligand. While there was a general trend for cytotoxicity to correlate with mustard reactivity, this was much less pronounced than with untargeted mustards. The compounds were ...

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