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Current Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Structure-Activity Relationships in The Acronycine Series

Author(s): Sylvie Michel, Elisabeth Seguin and Francois Tillequin

Volume 9, Issue 18, 2002

Page: [1689 - 1700] Pages: 12

DOI: 10.2174/0929867023369213

Price: $65

Abstract

Acronycine is active against a broad spectrum of solid tumors. Structure activity relationships demonstrated the crucial role of the 1,2-double bond. A hypothesis of bioactivation into 1,2-epoxide led to the development of a series of 1,2- dihydroxy-1,2-dihydroacronycine and 1,2-dihydroxy-1,2-dihydrobenzo[b]acronycine diesters that exhibited an increased potency when compared with the parent compound.

Keywords: acronycine, solid tumors, increased potency, antitumor activity, murine leukemia cell line, cytotoxic activity, catalytic osmic oxidation, enlarged spectrum


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