4.5 Article

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

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 11, Issue 9, Pages 1193-1196

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/S0960-894X(01)00190-1

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Funding

  1. NCI NIH HHS [CA-17625] Funding Source: Medline
  2. NIAID NIH HHS [AI-33066] Funding Source: Medline

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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. (C) 2001 Elsevier Science Ltd. all rights reserved.

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