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Studies directed toward the elucidation of the pharmacophore of steroid-based Sonic Hedgehog signaling inhibitors.
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2
Stereoselective synthesis of F-ring saturated estrone-derived inhibitors of Hedgehog signaling based on cyclopamine.
Org Lett. 2011 Sep 16;13(18):4786-9. doi: 10.1021/ol2017966. Epub 2011 Aug 15.
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Synthesis and biological evaluation of SANT-2 and analogues as inhibitors of the hedgehog signaling pathway.
Bioorg Med Chem. 2009 Jul 15;17(14):4943-54. doi: 10.1016/j.bmc.2009.06.008. Epub 2009 Jun 10.
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Sonic Hedgehog inhibition as a strategy to augment radiosensitivity of hepatocellular carcinoma.
J Gastroenterol Hepatol. 2015 Aug;30(8):1317-24. doi: 10.1111/jgh.12931.
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Cyclopamine-mediated hedgehog pathway inhibition depletes stem-like cancer cells in glioblastoma.
Stem Cells. 2007 Oct;25(10):2524-33. doi: 10.1634/stemcells.2007-0166. Epub 2007 Jul 12.
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Synthesis and biological evaluation of desmethylveramiline, a micromolar Hedgehog inhibitor.
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Sonic hedgehog signaling pathway is activated in ALK-positive anaplastic large cell lymphoma.
Cancer Res. 2009 Mar 15;69(6):2550-8. doi: 10.1158/0008-5472.CAN-08-1808. Epub 2009 Feb 24.

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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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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.
3
Design, synthesis, and biological evaluation of estrone-derived hedgehog signaling inhibitors.
Tetrahedron. 2011 Dec 30;67(52):10261-10266. doi: 10.1016/j.tet.2011.10.028.

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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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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.
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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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HEDGEHOG-GLI1 signaling regulates human glioma growth, cancer stem cell self-renewal, and tumorigenicity.
Curr Biol. 2007 Jan 23;17(2):165-72. doi: 10.1016/j.cub.2006.11.033. Epub 2006 Dec 28.
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Frequent requirement of hedgehog signaling in non-small cell lung carcinoma.
Oncogene. 2007 Feb 15;26(7):1046-55. doi: 10.1038/sj.onc.1209860. Epub 2006 Aug 14.
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Activation of the hedgehog pathway in advanced prostate cancer.
Mol Cancer. 2004 Oct 13;3:29. doi: 10.1186/1476-4598-3-29.
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Hedgehog signalling in prostate regeneration, neoplasia and metastasis.
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