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Synfacts 2008(11): 1127-1127  
DOI: 10.1055/s-0028-1083411
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart ˙ New York

Synthesis of (+)-Cortistatin A

Contributor(s): Philip Kocienski, Indu Dager
R. A. Shenvi, C. A. Guerrero, J. Shi, C.-C. Li, P. S. Baran*
The Scripps Research Institute, la jolla, USA
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Publikationsdatum:
23. Oktober 2008 (online)

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Significance

(+)-Cortistatin A inhibits the proliferation of human umbilical vein endothelial cells (HUVECs, IC50 = 1.8 nM) without showing any toxicity. This synthesis utilizes a novel hydroxyl-­directed dibromination of a methyl group (C → D) using AcOBr generated in situ.