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Bioorg Med Chem Lett. 2001 May 7;11(9):1193-6.

Antitumor agents. Part 204: synthesis and biological evaluation of substituted 2-aryl quinazolinones.

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  • 1Natural Products Laboratory, School of Pharmacy, University of North Carolina, Chapel Hill 27599, USA.


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.

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