SYNTHESIS AND PHARMACOLOGICAL ACTIVITY OF COMBRETASTATIN ANALOGS - NAPHTHYLCOMBRETASTATINS AND RELATED-COMPOUNDS

Authors
MEDARDE M DECLAIRAC RPL RAMOS AC CABALLERO E LOPEZ JL GRAVALOS DG SANFELICIANO A
Citation
M. Medarde et al., SYNTHESIS AND PHARMACOLOGICAL ACTIVITY OF COMBRETASTATIN ANALOGS - NAPHTHYLCOMBRETASTATINS AND RELATED-COMPOUNDS, Bioorganic & medicinal chemistry letters, 5(3), 1995, pp. 229-232
Citations number
18
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
3
Year of publication
1995
Pages
229 - 232
Database
ISI
SICI code
0960-894X(1995)5:3<229:SAPAOC>2.0.ZU;2-U
Abstract
Through a versatile synthesis of combretastatins we have prepared and assayed for activity some new compounds of this kind of antitumoral ag ents. Ketoderivatives (combretastatones) and other diphenylethane deri vatives display low activity, but naphthylcombretastatin 3e shows acti vity comparable to that of the most potent combretastatins-B (dihydroc ombretastatins), in spite of the lack of the 3-hydroxy-4-methoxyphenyl substructure considered to be neccesary for high antineoplastic poten cy.