Abstract
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.
Publication types
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Comparative Study
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology*
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Benzofurans / chemical synthesis*
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Benzofurans / chemistry
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Benzofurans / pharmacology*
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Benzopyrans / chemical synthesis*
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Benzopyrans / chemistry
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Benzopyrans / pharmacology*
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Cell Line, Tumor
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Cell Proliferation / drug effects*
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Crystallography, X-Ray
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Drug Screening Assays, Antitumor
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Furans / chemical synthesis*
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Furans / chemistry
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Furans / pharmacology*
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In Vitro Techniques
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Leukemia L1210 / drug therapy*
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Mice
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Models, Molecular
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Molecular Structure
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Naphthalenes / chemical synthesis
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Naphthalenes / chemistry
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Naphthalenes / pharmacology
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Structure-Activity Relationship
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src-Family Kinases / antagonists & inhibitors
Substances
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2-(4-oxo-1-benzopyran-3-ylmethylene)naphtho(2,1-b)furan-3-one
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Antineoplastic Agents
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Benzofurans
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Benzopyrans
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Furans
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Naphthalenes
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src-Family Kinases