Abstract
A series of 2',3',4',6,7-substituted 2-aryl quinazolinones were synthesized and evaluated for biological activity. Among them, 17 displayed significant growth inhibitory action against a panel of tumor cell lines. Compound 17 was also a potent inhibitor of tubulin polymerization. Compounds 8-10 displayed selective activity against P-gp-expressing epidermoid carcinoma of the asopharynx.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism
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Anti-HIV Agents / chemical synthesis
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Anti-HIV Agents / pharmacology
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / pharmacology*
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HIV Infections / drug therapy
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HIV Infections / virology
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Humans
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Lymphocytes / drug effects
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Lymphocytes / virology
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Quinazolines / chemical synthesis*
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Quinazolines / pharmacology*
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Structure-Activity Relationship
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Tubulin / biosynthesis
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Tubulin / drug effects
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Tumor Cells, Cultured
Substances
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ATP Binding Cassette Transporter, Subfamily B, Member 1
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Anti-HIV Agents
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Antineoplastic Agents
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Quinazolines
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Tubulin