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Synthesis of a 5-methylindolyl-containing macrocycle that displays ultrapotent Grb2 SH2 domain-binding affinity

  1. Author:
    Shi, Z. D.
    Lee, K.
    Wei, C. Q.
    Roberts, L. R.
    Worthy, K. M.
    Fisher, R. J.
    Burke, T. R.
  2. Author Address

    Burke, TR, NCI, Med Chem Lab, CCR, NIH, Ft Detrick, MD 21702 USA NCI, Med Chem Lab, CCR, NIH, Ft Detrick, MD 21702 USA. SAIC Frederick, Prot Chem Lab, Ft Detrick, MD 21702 USA.
    1. Year: 2004
  1. Journal: Journal of Medicinal Chemistry
    1. 47
    2. 4
    3. Pages: 788-791
  2. Type of Article: Article
  1. Abstract:

    The growth factor receptor-bound protein 2 (Grb2) is an SH2 domain-containing docking module that represents an attractive target for anticancer therapeutic intervention. Here, a ring-closing metathesis approach is utilized to synthesize a 5-methylindolyl-containing tetrapeptide mimetic (6) that exhibits unprecedented in vitro Grb2 SH2 domain-binding affinity (K-d = 93 pM). Key to the preparation of 6 is the enantioselective synthesis of (2S)-2-(3-(5-methylindolyl)methyl)pent-4-enylamine (12) as one of two ring-closing segments

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