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Preparation of Hymenialdisine, Analogues and Their Evaluation as Kinase Inhibitors

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The natural product hymenialdisine was first isolated in 1980 from the marine sponges of the genera Hymeniacidon, Acanthella, Axinella and Pseudaxinyssa. The structure was elucidated on the basis of X-ray crystallography demonstrating a structurally interesting pyrrole-azepin-8-one ring system bonded to a glycocyamidine ring. Great interest has been taken in synthesizing this type of scaffold due to its potent activity in competitive kinase inhibition. In addition, several patents have claimed pharmacological use of these compounds for prevention and treatment of different diseases. The challenging syntheses of hymenialdisine and its analogues are described in this review as well as their evaluation as kinase inhibitors.
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Keywords: Natural products; chemotherapy; hymenialdisine; kinase inhibitors; marine sponge metabolites

Document Type: Research Article

Affiliations: Department of Chemistry, College of Natural Sciences, Michigan State University, East Lansing, MI 48824, USA.

Publication date: 2009-08-01

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