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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Preparation of Hymenialdisine, Analogues and Their Evaluation as Kinase Inhibitors

Author(s): T. N.T. Nguyen and J. J. Tepe

Volume 16 , Issue 24 , 2009

Page: [3122 - 3143] Pages: 22

DOI: 10.2174/092986709788803015

Price: $65


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.

Keywords: Natural products, marine sponge metabolites, hymenialdisine, kinase inhibitors, chemotherapy

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