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Design and synthesis of a new, conformationally constrained, macrocyclic small-molecule inhibitor of STAT3 via 'click chemistry'

  1. Author:
    Chen, J. Y.
    Nikolovska-Coleska, Z.
    Yang, C. Y.
    Gomez, C.
    Gao, W.
    Krajewski, K.
    Jiang, S.
    Roller, P.
    Wang, S. M.

  2. Author Address

    Univ Michigan, Dept Internal Med, Ctr Comprehens Canc, Ann Arbor, MI 48109 USA. Univ Michigan, Dept Pharmacol & Med Chem, Ctr Comprehens Canc, Ann Arbor, MI 48109 USA. NCI, Med Chem Lab, NIH, Frederick, MD 21702 USA.;Wang, SM, Univ Michigan, Dept Internal Med, Ctr Comprehens Canc, Ann Arbor, MI 48109 USA.;shaomeng@umich.edu
    1. Year: 2007
    2. Date: Jul
  2. Journal: Bioorganic & Medicinal Chemistry Letters
    1. 17
    2. 14
    3. Pages: 3939-3942
  4. Type of Article: Article
  5. ISSN: 0960-894X
  1. Abstract:

    STAT3 is a promising molecular target for the design of new anticancer drugs. In this paper, we report the design and synthesis of a conformationally constrained macrocyclic peptidomimetic 2 via click chemistry. Compound 2 was determined to bind to STAT3 with a K, value of 7.3 mu M in a competitive fluorescence-polarization-based binding assay, representing a promising initial lead compound for further optimization. (C) 2007 Elsevier Ltd. All rights reserved.

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External Sources

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  2. DOI: 10.1016/j.bmcl.2007.04.096
  3. View record in Web of Science®
  4. WOS: 000248074600026

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