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Synthesis and Biological Evaluation of 2-Acyl Analogues of Paclitaxel (Taxol)

  1. Author:
    Kingston, D. G. I.
    Chaudhary, A. G.
    Chordia, M. D.
    Gharpure, M.
    Gunatilaka, A. A. L.
    Higgs, P. I.
    Rimoldi, J. M.
    Samala, L.
    Jagtap, P. C.
    Giannakakou, P.
    Jiang, Y. Q.
    Lin, C. M.
    Hamel, E.
    Long, B. H.
    Fairchild, C. R.
    Johnston, K. A.

  2. Author Address

    Kingston DGI VIRGINIA POLYTECH INST & STATE UNIV DEPT CHEM BLACKSBURG, VA 24061 USA NCI DIV CLIN SCI MED BRANCH NIH BETHESDA, MD 20892 USA NCI FREDERICK CANC RES & DEV CTR DIV CANC TREATMENT & DIAG DEV THERAPEUT PROGRAM FREDERICK, MD 21702 USA BRISTOL MYERS SQUIBB PHARMACEUT RES INST PRINCETON, NJ USA
    1. Year: 1998
  2. Journal: Journal of Medicinal Chemistry
    1. 41
    2. 19
    3. Pages: 3715-3726
  4. Type of Article: Article
  1. Abstract:

    The anticancer drug paclitaxel (Taxol) has been converted to a large number of 2-debenzoyl-2-aroyl derivatives by three different methods. The bioactivities of the resulting analogues were determined in both tubulin polymerization and cytotoxicity assays, and several analogues with enhanced activity as compared with paclitaxel were discovered. Correlation of cytotoxicity in three cell lines with tubulin polymerization activity showed reasonable agreement. Among the cell lines examined, the closest correlation with antitubulin activity was observed with a human ovarian carcinoma cell line. [References: 53]

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