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Synthesis and Biological Activity of a-Nor-Paclitaxel Analogues

  1. Author:
    Chordia, M. D.
    Kingston, D. G. I.
    Hamel, E.
    Lin, C. M.
    Long, B. H.
    Fairchild, C. A.
    Johnston, K. A.
    Rose, W. C.

  2. Author Address

    Chordia MD VIRGINIA POLYTECH INST & STATE UNIV DEPT CHEM BLACKSBURG, VA 24061 USA NCI FREDERICK CANC RES & DEV CTR LAB DRUG DISCOVERY RES & DEV DEV THERAPEUT PROGRAM FREDERICK, MD 21702 USA BRISTOL MYERS SQUIBB PHARMACEUT RES INST PRINCETON, NJ 08543 USA
    1. Year: 1997
  2. Journal: Bioorganic & Medicinal Chemistry
    1. 5
    2. 5
    3. Pages: 941-947
  4. Type of Article: Article
  1. Abstract:

    A number of paclitaxel analogues with a 5-membered A-ring (A-nor-paclitaxels, or (15 right-arrow 1)-abeo-paclitaxels) have been prepared in order to determine whether analogues of this class might have improved bioactivity as compared with paclitaxel. Most of the compounds synthesized were less active than paclitaxel, but one analogue was equivalent to paclitaxel in a tubulin-assembly assay, and another analogue was more cytotoxic than paclitaxel in two different cell lines of the NCI screen. [References: 13]

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