Structure-Activity Relationships in The Acronycine Series

Sylvie      Michel; Elisabeth      Seguin; Francois      Tillequin

doi:10.2174/0929867023369213

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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Current Medicinal Chemistry

Title: Structure-Activity Relationships in The Acronycine Series

Volume: 9 Issue: 18

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

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

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.

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Michel Sylvie, Seguin Elisabeth and Tillequin Francois, Structure-Activity Relationships in The Acronycine Series, Current Medicinal Chemistry 2002; 9 (18) . https://dx.doi.org/10.2174/0929867023369213