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 nasopharynx.
