SYNTHESIS AND EVALUATION OF NOVEL 3,4-EPOXYPIPERIDINES AS EFFICIENT DNA ALKYLATING AGENTS

摘要

3,4-Epoxypiperidine derivatives are novel DNA alkylating agents based on an active site of the antitumor antibiotics azinomycins A and B. A 3,4-epoxypiperidine library was constructed containing derivatives with a variety of functional groups at C5 via Huisgen reaction, and DNA cleavage activity was examined. Results revealed a more active derivative than any 3,4-epoxypiperidines previously reported.