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

  1. Author:
    Xia, Y.
    Yang, Z. Y.
    Hour, M. J.
    Kuo, S. C.
    Xia, P.
    Bastow, K. F.
    Nakanishi, Y.
    Nampoothiri, P.
    Hackl, T.
    Hamel, E.
    Lee, K. H.

  2. Author Address

    Univ N Carolina, Sch Pharm, Nat Prod Lab, Chapel Hill, NC 27599 USA. Univ N Carolina, Sch Pharm, Nat Prod Lab, Chapel Hill, NC 27599 USA. China Med Coll, Taichung, Taiwan. NCI, Frederick Canc Res & Dev Ctr, Screening Technol Branch, Dev Therapeut Program, Div Canc Treatment & Diag, Frederick, MD 21702 USA. Lee KH Univ N Carolina, Sch Pharm, Nat Prod Lab, Chapel Hill, NC 27599 USA.
    1. Year: 2001
  2. Journal: Bioorganic & Medicinal Chemistry Letters
    1. 11
    2. 9
    3. Pages: 1193-1196
  4. Type of Article: Article
  1. 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 nasopharynx. (C) 2001 Elsevier Science Ltd. all rights reserved.

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