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Antitumor agents. Part 186: Synthesis and biological evaluation of demethylcolchiceinamide analogues as cytotoxic DNA topoisomerase II inhibitors

  1. Author:
    Guan, J.
    Zhu, X. K.
    Tachibana, Y.
    Bastow, K. F.
    Brossi, A.
    Hamel, E.
    Lee, K. H.

  2. Author Address

    Lee KH Univ N Carolina, Sch Pharm, Div Med Chem & Nat Prod, Nat Prod Lab Chapel Hill, NC 27599 USA Univ N Carolina, Sch Pharm, Div Med Chem & Nat Prod, Nat Prod Lab Chapel Hill, NC 27599 USA NCI, Frederick Canc Res & Dev Ctr, Div Canc Treatment Diagnosis & Ctr, Dev Therapeut Program,Lab Drug Discovery Res & De Ft Detrick, MD 21702 USA
    1. Year: 1998
  2. Journal: Bioorganic & Medicinal Chemistry
    1. 6
    2. 11
    3. Pages: 2127-2131
  4. Type of Article: Article
  1. Abstract:

    Demethylation of colchiceinamide (2) and its analogues (3-10) afforded a novel class of mammalian DNA topoisomerase II inhibitors (2a-10a) without displaying tubulin inhibitory activity. All target compounds inhibited the catalytic activity of topoisomerase II at drug concentrations at 100 mu M. An in vitro cytotoxicity assay indicated that compounds 3a and 8a were strong and tissue-selective cytotoxic agents against the MCF-7 breast cancer cell line (IC50 = 0.36 and 0.48 mu g/mL, respectively) and the CAKI-1 renal cancer cell line (IC50 = 0.72 and 0.96 mu g/mL, respectively). (C) 1998 Elsevier Science Ltd. All rights reserved. [References: 16]

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