Bioorganic & medicinal chemistry

… N-methyl amide and simple ester replacement for the l-histidine secondary amide: Direct functional characterization of the requirement for secondary amide metal …

DL Boger, S Teramoto, H Cai

Index: Boger, Dale L.; Teramoto, Shuji; Cai, Hui Bioorganic and Medicinal Chemistry, 1996 , vol. 4, # 2 p. 179 - 193

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Citation Number: 21

Abstract

The synthesis and comparative examination of 3–5, analogues of deglycobleomycin A2 (2) which address the inferred importance of the l-histidine secondary amide directly, are detailed. The agent 3 lacks only the l-histidine β-hydroxy group of deglycobleomycin A2 and the corresponding agents 4 and 5 incorporate a tertiary N-methyl amide and simple ester in place of the l-histidine secondary amide. The DNA cleavage properties of 3 proved ...