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Total Synthesis and Biological Evaluation of Largazole and Derivatives with Promising Selectivity for Cancers Cells

  1. Author:
    Zeng, X.
    Yin, B. L.
    Hu, Z.
    Liao, C. Z.
    Liu, J. L.
    Li, S.
    Li, Z.
    Nicklaus, M. C.
    Zhou, G. B.
    Jiang, S.

  2. Author Address

    [Zeng, Xin; Hu, Zheng; Liu, Jinglei; Li, Shang; Zhou, Guangbiao; Jiang, Sheng] CAS, Guangzhou Inst Biomed & Hlth, Guangzhou 510663, Guangdong, Peoples R China. [Hu, Zheng; Liu, Jinglei; Zhou, Guangbiao] CAS, Lab Mol Carcinogenesis & Targeted Therapy Canc, State Key Lab Biomembrane & Membrane Biotechnol, Inst Zool, Beijing 100101, Peoples R China. [Yin, Biaolin] S China Univ Technol, Guangzhou 510640, Peoples R China. [Liao, Chenzhong; Nicklaus, Marc C.] NCI, NIH, Frederick, MD 21702 USA. [Hu, Zheng; Liu, Jinglei; Zhou, Guangbiao] Univ Sci & Technol China, Hefei 230027, Peoples R China. [Li, Zheng] Methodist Hosp, Res Inst, Houston, TX 77030 USA.;Zhou, GB, CAS, Guangzhou Inst Biomed & Hlth, Guangzhou 510663, Guangdong, Peoples R China.;gbzhou@ioz.ac.cn jiang_sheng@gibh.ac.cn
    1. Year: 2010
    2. Date: Mar
  2. Journal: Organic Letters
    1. 12
    2. 6
    3. Pages: 1368-1371
  4. Type of Article: Article
  5. ISSN: 1523-7060
  1. Abstract:

    The efficient total synthesis of the natural substance largazole is described. Using this strategy, a small library of largazole analogs was developed. Structure-activity relationship studies suggested that the geometry of the alkene In the side chain is critical. While the largazole's analogues with trans-alkene are potent for the anti proliferative effect, those with cls-alkene are completely inactive. Most importantly, replacement of valine with tyrosine in largazole increased selectivity toward human cancer cells over human normal cells more than 100-fold.

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External Sources

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  2. DOI: 10.1021/ol100308a
  3. View record in Web of Science®
  4. WOS: 000275379100057

Library Notes

  1. Fiscal Year: FY2009-2010
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