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Antitumor agents. Part 236: Synthesis of water-soluble colchicine derivatives

  1. Author:
    Nakagawa-Goto, K.
    Chen, C. X.
    Hamel, E.
    Wu, C. C.
    Bastow, K. F.
    Brossi, A.
    Lee, K. H.

  2. Author Address

    Univ N Carolina, Sch Pharm, Nat Prod Lab, Chapel Hill, NC 27599 USA. NCI, Screening Technol Branch, Dev Therapeut Program, Div Canc Treatment & Diagnosis, Ft Detrick, MD 21702 USA Lee, KH, Univ N Carolina, Sch Pharm, Nat Prod Lab, Chapel Hill, NC 27599 USA
    1. Year: 2005
    2. Date: JAN 3
  2. Journal: Bioorganic & Medicinal Chemistry Letters
    1. 15
    2. 1
    3. Pages: 235-238
  4. Type of Article: Article
  1. Abstract:

    Water-soluble colchicine derivatives were synthesized from 2-demethylcolchicine and 2-demethylthiocolchicine and evaluated in vitro against human tumor cell replication and for inhibition of tubulin polymerization. The glycinate esters (4, 5) and their tartaric acid salts (4a, 5a) showed potent cytotoxic activity in three different tumor cell lines with IC50 values ranging from 0.02 to 0.88 mug/mL. The thiocolchicine analogs (5, 5a) were more potent than the colchicine analogs (4, 4a) in the tubulin polymerization assay. In particular, the water-soluble salt 5a merits preclinical development as an antitumor agent. (C) 2004 Elsevier Ltd. All rights reserved

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External Sources

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  2. DOI: 10.1016/j.bmcl.2004.07.098
  3. View record in Web of Science®
  4. WOS: 000225773600045

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