Abstract
A series of aroylnaphthalene derivatives were prepared as bioisosteres of combrestatin A-4 and evaluated for anticancer activity. 2-Amino-1-aroylnaphthalene and 2-hydroxy-1-aroylnaphthalene, 9 and 8, respectively, showed strong antiproliferative activity with IC(50) values of 2.1-26.3 nM against a panel of human cancer cell lines including multiple-drug resistant cell line. Compound 9 demonstrated better antiproliferative activity and has a comparable tubulin binding efficacy as that of colchicine.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Anisoles / chemical synthesis*
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Anisoles / pharmacology
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Cell Line, Tumor
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Cell Proliferation
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Chemistry, Pharmaceutical / methods*
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Drug Design
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Drug Screening Assays, Antitumor
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Humans
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Indoles / chemistry
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Inhibitory Concentration 50
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Models, Chemical
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Naphthalenes / chemical synthesis*
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Naphthalenes / chemistry
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Naphthalenes / pharmacology
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Neoplasms / drug therapy*
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Structure-Activity Relationship
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Tubulin / chemistry*
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Tubulin Modulators / chemical synthesis*
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Tubulin Modulators / pharmacology
Substances
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Anisoles
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Indoles
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Naphthalenes
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Tubulin
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Tubulin Modulators
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naphthalene