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Conformationally constrained analogues of diacylglycerol. 18. The incorporation of a hydroxamate moiety into diacylglycerol- lactones reduces lipophilicity and helps discriminate between sn-1 and sn-2 binding modes to protein kinase c (PK-C). Implications for isozyme specificity

  1. Author:
    Lee, J.
    Han, K. C.
    Kang, J. H.
    Pearce, L. L.
    Lewin, N. E.
    Yan, S. Q.
    Benzaria, S.
    Nicklaus, M. C.
    Blumberg, P. M.
    Marquez, V. E.

  2. Author Address

    Seoul Natl Univ, Coll Pharm, Med Chem Lab, Kwanak Ku, Seoul 151742, South Korea. Seoul Natl Univ, Coll Pharm, Med Chem Lab, Kwanak Ku, Seoul 151742, South Korea. NCI, Cellular Carcinogenesis & Tumor Promot Lab, Ctr Canc Res, Bethesda, MD 20892 USA. NCI, Med Chem Lab, Ctr Canc Res, Frederick, MD 21701 USA. Lee J Seoul Natl Univ, Coll Pharm, Med Chem Lab, Kwanak Ku, Seoul 151742, South Korea.
    1. Year: 2001
  2. Journal: Journal of Medicinal Chemistry
    1. 44
    2. 25
    3. Pages: 4309-4312
  4. Type of Article: Letter
  1. Abstract:

    An approach to reduce the log P in a series of diacylglycerol (DAG)-lactones known for their high binding affinity for protein kinase C (PK-C) is presented. Branched alkyl groups with reduced lipophilicity were selected and combined with the replacement of the ester or lactone oxygens by NH or NOH groups. Compound 6a with an isosteric N-hydroxyl amide arm represents the most potent and least lipophilic DAG analogue known to date.

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