4.7 Article

9,10-Secosteroids, protein kinase inhibitors from the Chinese gorgonian Astrogorgia sp.

Journal

BIOORGANIC & MEDICINAL CHEMISTRY
Volume 19, Issue 22, Pages 6873-6880

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2011.09.028

Keywords

Gorgonian; Astrogorgia sp.; 9,10-Secosteroids; Structural elucidation; Protein kinase inhibition

Funding

  1. NSFC [30930109]
  2. National Key Innovation Project [2011AA090701, 2009ZX09501-014, 2009ZX09103-140, 201005022-4]
  3. International Cooperation Projects [2010DFA31610]

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Fourteen new 9,10-secosteroids designated as astrogorgols A-N (1-14) were isolated from a Chinese gorgonian Astrogorgia sp. together with eight known analogues. The structural patterns were characterized by the presence of a sterol-based 9,10-seco nucleus containing a 3-hydroxy-10-methylphenyl ring. Astrogorgol N (14) possessing a 1,4-dien-3-one unit in ring A was biogenetically considered as an intermediate to generate diverse 9,10-secosteroids. Five compounds showed significant inhibitory activities against human tumor related protein kinases, including ALK, AXL, FAK, IGF-1R, MET wt, SRC, and VEGF-R2. (C) 2011 Elsevier Ltd. All rights reserved.

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