Synthesis and primary cytotoxicity evaluation of arylmethylenenaphthofuranones derivatives

New series of 2(or 3)-arylmethylenenaphtho[2,1-b]furan-3(or 2)-ones were synthesized, characterized and tested for anticancer properties in vitro. The target compounds were prepared by Knoevenagel coupling between the naphthofuranones 3, 28-30 and formyl derivatives. 2-(4-Oxo-1-benzopyran-3-ylmethyl...

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Bibliographic Details
Published in:	Journal of enzyme inhibition and medicinal chemistry Vol. 21; no. 3; p. 313
Main Authors:	Lardic, Morgane, Patry, Cedric, Duflos, Muriel, Guillon, Jean, Massip, Stephane, Cruzalegui, Francisco, Edmonds, Thomas, Giraudet, Stephanie, Marini, Laetitia, Leonce, Stephane
Format:	Journal Article
Language:	English
Published:	England 01-01-2006
Subjects:	Animals Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Benzofurans - chemical synthesis Benzofurans - chemistry Benzofurans - pharmacology Benzopyrans - chemical synthesis Benzopyrans - chemistry Benzopyrans - pharmacology Cell Line, Tumor Cell Proliferation - drug effects Crystallography, X-Ray Drug Screening Assays, Antitumor Furans - chemical synthesis Furans - chemistry Furans - pharmacology In Vitro Techniques Leukemia L1210 - drug therapy Mice Models, Molecular Molecular Structure Naphthalenes - chemical synthesis Naphthalenes - chemistry Naphthalenes - pharmacology src-Family Kinases - antagonists & inhibitors Structure-Activity Relationship
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Summary:	New series of 2(or 3)-arylmethylenenaphtho[2,1-b]furan-3(or 2)-ones were synthesized, characterized and tested for anticancer properties in vitro. The target compounds were prepared by Knoevenagel coupling between the naphthofuranones 3, 28-30 and formyl derivatives. 2-(4-Oxo-1-benzopyran-3-ylmethylene)naphtho[2,1-b]furan-3-one 36 was the most active compound (IC50 (L1210) = 1.6 microM). These compounds were also evaluated, in an independent manner, as inhibitors of Src protein tyrosine kinase, but only minor activity was observed.
ISSN:	1475-6366
DOI:	10.1080/14756360600741834