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Current Pharmaceutical Design


ISSN (Print): 1381-6128
ISSN (Online): 1873-4286

One Hundred Faces of Cyclopamine

Author(s): Valentina Iovine, Mattia Mori, Andrea Calcaterra, Simone Berardozzi and Bruno Botta

Volume 22, Issue 12, 2016

Page: [1658 - 1681] Pages: 24

DOI: 10.2174/1381612822666160112130157

Price: $65


The natural steroidal alkaloid cyclopamine has been identified as the first inhibitor of the Hedgehog (Hh) signaling pathway, which is implicated in embryonic development and tumorigenesis, as well as is hyperactivated in cancer stem cells (CSCs). The list of Hh-dependent tumors is steadily growing, and it has been estimated that about 25% of all cancer deaths show signs of aberrant Hh pathway activation. Notably, cyclopamine has been found to exert anticancer activity against several types of human cancer and to inhibit CSCs proliferation, thus highlighting the druggability of the Hh pathway and paving new opportunities in anticancer drug discovery. The aim of the present work is to review the main synthetic strategies to cyclopamine and its derivatives, with particular emphasis on the challenging chemical modifications aimed at improving the biological activity of the molecule.

Keywords: Cyclopamine, hedgehog pathway, anticancer, organic synthesis, C-nor-D-homosteroid, Veratrum alkaloids.

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