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Stereoselective synthesis of F-ring saturated estrone-derived inhibitors of Hedgehog signaling based on cyclopamine.
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Exo-cyclopamine--a stable and potent inhibitor of hedgehog-signaling.
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Semisynthetic cyclopamine analogues as potent and orally bioavailable hedgehog pathway antagonists.
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Discovery of a potent and orally active hedgehog pathway antagonist (IPI-926).
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Synthesis of cyclopamine using a biomimetic and diastereoselective approach.
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One Hundred Faces of Cyclopamine.
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Cyclopamine bioactivity by extraction method from Veratrum californicum.
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Studies directed toward the elucidation of the pharmacophore of steroid-based Sonic Hedgehog signaling inhibitors.
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Syntheses and medicinal chemistry of spiro heterocyclic steroids.
Beilstein J Org Chem. 2024 Jul 24;20:1713-1745. doi: 10.3762/bjoc.20.152. eCollection 2024.
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Convergent Total Synthesis of (-)-Cyclopamine.
J Am Chem Soc. 2023 Oct 11;145(40):21760-21765. doi: 10.1021/jacs.3c09085. Epub 2023 Oct 2.
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Ligand-Controlled Palladium-Catalyzed Carbonylation of Alkynols: Highly Selective Synthesis of α-Methylene-β-Lactones.
Angew Chem Int Ed Engl. 2020 Nov 23;59(48):21585-21590. doi: 10.1002/anie.202006550. Epub 2020 Sep 17.
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Design of Hedgehog pathway inhibitors for cancer treatment.
Med Res Rev. 2019 May;39(3):1137-1204. doi: 10.1002/med.21555. Epub 2018 Nov 28.
6
C-H-Functionalization logic guides the synthesis of a carbacyclopamine analog.
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1
Synthesis and biological evaluation of desmethylveramiline, a micromolar Hedgehog inhibitor.
Bioorg Med Chem Lett. 2011 Jun 15;21(12):3608-12. doi: 10.1016/j.bmcl.2011.04.103. Epub 2011 Apr 29.
2
Exo-cyclopamine--a stable and potent inhibitor of hedgehog-signaling.
Chem Commun (Camb). 2011 Jul 14;47(26):7362-4. doi: 10.1039/c1cc11782c. Epub 2011 May 17.
3
Companies race to develop first Hedgehog inhibitor cancer drug.
Nat Med. 2011 May;17(5):523. doi: 10.1038/nm0511-523.
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Childhood medulloblastoma: novel approaches to the classification of a heterogeneous disease.
Acta Neuropathol. 2010 Sep;120(3):305-16. doi: 10.1007/s00401-010-0726-6. Epub 2010 Jul 23.
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Genentech obtains proof of concept for hedgehog inhibition.
Nat Biotechnol. 2009 Nov;27(11):968-9. doi: 10.1038/nbt1109-968.
9
Semisynthetic cyclopamine analogues as potent and orally bioavailable hedgehog pathway antagonists.
J Med Chem. 2008 Nov 13;51(21):6646-9. doi: 10.1021/jm8008508. Epub 2008 Oct 9.
10
Melanomas require HEDGEHOG-GLI signaling regulated by interactions between GLI1 and the RAS-MEK/AKT pathways.
Proc Natl Acad Sci U S A. 2007 Apr 3;104(14):5895-900. doi: 10.1073/pnas.0700776104. Epub 2007 Mar 28.

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