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

Daowan Lai; Shanjiang Yu; Leen van Ofwegen; Frank Totzke; Peter Proksch; Wenhan Lin

doi:10.1016/j.bmc.2011.09.028

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

Bioorg Med Chem. 2011 Nov 15;19(22):6873-80. doi: 10.1016/j.bmc.2011.09.028. Epub 2011 Sep 21.

Authors

Daowan Lai¹, Shanjiang Yu, Leen van Ofwegen, Frank Totzke, Peter Proksch, Wenhan Lin

Affiliation

¹ State Key Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing, PR China.

PMID: 21982797
DOI: 10.1016/j.bmc.2011.09.028

Abstract

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Anthozoa / chemistry*
Cell Line, Tumor
Drug Screening Assays, Antitumor
Humans
Protein Kinase Inhibitors / chemistry*
Protein Kinase Inhibitors / isolation & purification
Protein Kinase Inhibitors / pharmacology
Secosteroids / chemistry*
Secosteroids / isolation & purification
Secosteroids / pharmacology

Substances

Protein Kinase Inhibitors
Secosteroids