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6-alkylamino- and 2,3-dihydro-3 '-methoxy-2-phenyl-4- quinazolinones and related compounds: Their synthesis, cytotoxicity, and inhibition of tubulin polymerization

  1. Author:
    Hour, M. J.
    Huang, L. J.
    Kuo, S. C.
    Xia, Y.
    Bastow, K.
    Nakanishi, Y.
    Hamel, E.
    Lee, K. H.

  2. Author Address

    China Med Coll, Grad Inst Pharmaceut Chem, Taichung, Taiwan. China Med Coll, Grad Inst Pharmaceut Chem, Taichung, Taiwan. Univ N Carolina, Sch Pharm, Div Med Chem & Nat Prod, Chapel Hill, NC 27599 USA. NCI, Frederick Canc Res & Dev Ctr, Div Canc Treatment & Diag, Dev Therapeut Program, Screening Technol Branch, Frederick, MD 21702 USA.
    1. Year: 2000
  2. Journal: Journal of Medicinal Chemistry
    1. 43
    2. 23
    3. Pages: 4479-4487
  4. Type of Article: Article
  1. Abstract:

    As part of our continuing search for potential anticancer candidates among 2-phenyl-4-quinolones and 2-phenyl-4- quinazolinones, two series of 6,7,2',3',4',5'-substituted 2- phenyl-4-quinazolinones and 6,2',3',4',5'-substituted 2,3- dihydro-2-phenyl-4-quinazolinones were synthesized and evaluated for cytotoxicity and as inhibitors of tubulin polymerization. In general, a good correlation was found between the two activities. Five of the 6-substituted heterocyclic 2-phenyl-4-quinozolinones (37-51) showed significant cytotoxicity against a panel of human tumor cell lines with EC50 values in the low micromolar to nanomolar concentration ranges. Compound 38 was the most potent of these compounds, as well as the most potent inhibitor of tubulin polymerization in this series. The activity of 38 was in the same range as those of the antimitotic natural products, colchicine, podophyllotoxin, and combretastatin A-4. Substituted 2-phenyl-4-quinazolinones and 2,3-dihydro-2-phenyl- 4-quinazolinones also displayed highly selective cytotoxicity against the ovarian cancer 1A9 and P-gp resistant KB-VIN cell lines.

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