Title: Structure-Activity Relationships in The Acronycine Series
VOLUME: 9 ISSUE: 18
Author(s):Sylvie Michel, Elisabeth Seguin and Francois Tillequin
Affiliation:Laboratoire de Pharmacognosie de l'Universite Rene Descartes, U.M.R. / C.N.R.S.n 8638, Faculte des Sciences Pharmaceutiques et Biologiques, 4, Avenuede l'Observatoire, F-75006 Paris, France
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.
