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Design, synthesis, and biological evaluation of estrone-derived hedgehog signaling inhibitors
Authors:Winkler Jeffrey D  Isaacs André K  Xiang Chaomei  Baubet Valérie  Dahmane Nadia
Affiliation:a Department of Chemistry, University of Pennsylvania, Philadelphia, PA 19104, USA
b The Wistar Institute, Philadelphia, PA 19104, USA
Abstract:
The design, synthesis, and biological evaluation of new analogs of the naturally occurring compound cyclopamine, a hedgehog signaling inhibitor, are described. Structure-activity relationship studies lead to an evolving model for the pharmacophore of this medically promising compound class of anti-cancer chemotherapeutic agents.
Keywords:Cyclopamine   Steroidal alkaloid   Cancer chemotherapy   Hedgehog signaling   Structure-activity relationships
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