Synthesis and evaluation of novel ellipticines as potential anti-cancer agents

FM Deane, EC O'Sullivan, AR Maguire…

Index: Deane, Fiona M.; O'Sullivan, Elaine C.; Maguire, Anita R.; Gilbert, Jayne; Sakoff, Jennette A.; McCluskey, Adam; McCarthy, Florence O. Organic and Biomolecular Chemistry, 2013 , vol. 11, # 8 p. 1334 - 1344

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Citation Number: 21

Abstract

Drugs that inhibit DNA topoisomerase I and DNA topoisomerase II have been widely used in cancer chemotherapy. We report herein the results of a focused medicinal chemistry effort around novel ellipticinium salts which target topoisomerase I and II enzymes with improved solubility. The salts were prepared by reaction of ellipticine with the required alkyl halide and evaluated for DNA intercalation, topoisomerase inhibition and growth inhibition against 12 ...