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Identification and structure-activity relationships of ortho-biphenyl carboxamides as potent Smoothened antagonists inhibiting the Hedgehog signaling pathway.

Peukert, Stefan and Jain, Rishi and Geisser, Adrian and Sun, Yingchuan and Zhang, Rui and Bourret, Aaron and Carlson, Adam and Dasilva, Jennifer and Ramamurthy, Arun and Kelleher Iii, Joseph (2009) Identification and structure-activity relationships of ortho-biphenyl carboxamides as potent Smoothened antagonists inhibiting the Hedgehog signaling pathway. Bioorganic & Medicinal Chemistry Letters, 19 (2). pp. 328-331. ISSN 1464-3405

Abstract

Ortho-biphenyl carboxamides, originally prepared as inhibitors of microsomal triglyceride transfer protein (MTP) have been identified as novel inhibitors of the Hedgehog signaling pathway. Structure-activity relationship studies for this class of compounds reduced MTP inhibitory activity and led to low nanomolar Hedgehog inhibitors. Binding assays revealed that the compounds act as antagonists of Smoothened and show cross-reactivity for both the human and mouse receptor.

Item Type: Article
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Additional Information: author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
Keywords: Hedgehog inhibitor; Smoothened antagonist; Antiproliferative agent; SAR
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Date Deposited: 14 Dec 2009 13:48
Last Modified: 31 Jan 2013 00:53
URI: https://oak.novartis.com/id/eprint/1494

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