Design, synthesis, and evaluation of DNA minor groove binding agents: The duocarmycins

Abstract

A summary of recent investigations of the duocarmycins is provided including the total synthesis of (+)-and ent-(−)-duocarmycin SA, the preparation and evaluation of the minimum potent pharmacophore of the alkylation subunit constituting the common pharmacophore of duocarmycin A and SA, the definition and characterization of the DNA alkylation properties of the agents and their correlation with biological properties, and studies to define the fundamental reactivity and molecular recognition principles relating the agents structure and properties. © 1994, Walter de Gruyter. All rights reserved.