• Title of article

    Synthesis and Biological Evaluation of 2-Indolyloxazolines as a New Class of Tubulin Polymerization Inhibitors. Discovery of A-289099 as an Orally Active Antitumor Agent

  • Author/Authors

    Qun Li ، نويسنده , , Keith W. Woods، نويسنده , , Akiyo Claiborne، نويسنده , , Stephen L. Gwaltney II، نويسنده , , Kenneth J. Barr، نويسنده , , Gang Liu، نويسنده , , Laura Gehrke، نويسنده , , R. Bruce Credo، نويسنده , , Yu Hua Hui، نويسنده , , Jang Lee، نويسنده , , Robert B. Warner، نويسنده , , Peter Kovar، نويسنده , , Michael A. Nukkala، نويسنده , , Nicolette A. Zielinski، نويسنده , , Stephen K. Tahir، نويسنده , , Michael Fitzgerald، نويسنده , , Ki H. Kim، نويسنده , , Kennan Marsh، نويسنده , , David Frost، نويسنده , , Shi-Chung Ng، نويسنده , , et al.، نويسنده ,

  • Issue Information
    روزنامه با شماره پیاپی سال 2002
  • Pages
    5
  • From page
    465
  • To page
    469
  • Abstract
    A series of indole containing oxazolines has been discovered as a result of structural modifications of the lead compound A-105972. The compounds exert their anticancer activity through inhibition of tubulin polymerization by binding at the colchicine site. A-289099 was identified as an orally active antimitotic agent active against various cancer cell lines including those that express the MDR phenotype. The anticancer activity, pharmacokinetics, and an efficient and enantioselective synthesis of A-289099 are described.
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Serial Year
    2002
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Record number

    791997