Tetrahedron

Man-designed bleomycins. synthesis of dioxygen activating molecules and a DNA cleaving molecule based on bleomycin-Fe (II)-0 2 complex

A Kittaka, Y Sugano, M Otsuka, M Ohno

Index: Kittaka; Sugano; Otsuka; Ohno Tetrahedron, 1988 , vol. 44, # 10 p. 2821 - 2833

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Citation Number: 42

Abstract

A synthetic model for the metal binding site of bleomycin with a 4-methoxypyridine nucleus and atert-butyl group is shown to be comparable to bleomycin in terms of dioxygen activation. This model ligand is coupled with a DNA affinity moiety, tetrapeptide S, to afford a mandesigned bleomycin which exhibits potent DNA cleaving activityin vitro.