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Hedgehog pathway inhibitors: a patent review (2009 – present)

Pages 345-361 | Published online: 08 Jan 2013

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Fabrizio Manetti & Elena Petricci. (2016) Evaluation of WO2014207069 A1: Multitarget Hedgehog pathway inhibitors and uses thereof. Expert Opinion on Therapeutic Patents 26:4, pages 529-535.
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Aiwu Ruth He, Daniel C Smith & Lopa Mishra. (2015) Targeting cancer stem cells in hepatocellular carcinoma. Gastrointestinal Cancer: Targets and Therapy 5, pages 1-10.
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Minhang Xin. (2015) Hedgehog inhibitors: a patent review (2013 – present). Expert Opinion on Therapeutic Patents 25:5, pages 549-565.
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Stephen E Gould, Jennifer A Low, James C Marsters$suffix/text()$suffix/text(), Kirk Robarge, Lee L Rubin, Frederic J de Sauvage, Daniel P Sutherlin, Harvey Wong & Robert L Yauch. (2014) Discovery and preclinical development of vismodegib. Expert Opinion on Drug Discovery 9:8, pages 969-984.
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Franciszek Sączewski & Łukasz Balewski. (2013) Biological activities of guanidine compounds, 2008 – 2012 update. Expert Opinion on Therapeutic Patents 23:8, pages 965-995.
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Wentian Yang & Benjamin G Neel. (2013) From an orphan disease to a generalized molecular mechanism. Rare Diseases 1:1.
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Jiachen Wen & M. Kyle Hadden. (2021) Medulloblastoma drugs in development: Current leads, trials and drawbacks. European Journal of Medicinal Chemistry 215, pages 113268.
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Raíza Dias Freitas, Rosane Borges Dias, Manuela Torres Andion Vidal, Ludmila de Faro Valverde, Rafaela Gomes Alves Costa, Andresa Karen Andrade Damasceno, Caroline Brandi Schlaepfer Sales, Leonardo de Oliveira Siquara da Rocha, Mitermayer Galvão dos Reis, Milena Botelho Pereira Soares, Ricardo Della Coletta, Thiago Almeida Pereira, Daniel Pereira Bezerra & Clarissa Araújo Gurgel Rocha. (2020) Inhibition of CAL27 Oral Squamous Carcinoma Cell by Targeting Hedgehog Pathway With Vismodegib or Itraconazole. Frontiers in Oncology 10.
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Yanan Chang, Hong Chen, Jie Duan, Wang Wu, Fangshu Le & Fen Mou. (2020) The inhibitory effect and safety of GANT61 on HeLa cells in nude mice. Experimental and Molecular Pathology 113, pages 104352.
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Nil Kiliç, Yasemin Ö. Islakoğlu, İlker Büyük, Bala Gür-Dedeoğlu & Demet Cansaran-Duman. (2019) Determination of Usnic Acid Responsive miRNAs in Breast Cancer Cell Lines. Anti-Cancer Agents in Medicinal Chemistry 19:12, pages 1463-1472.
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Jitender Bariwal, Virender Kumar, Yuxiang Dong & Ram I. Mahato. (2018) Design of Hedgehog pathway inhibitors for cancer treatment. Medicinal Research Reviews 39:3, pages 1137-1204.
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Qin Chen, Haoran Zhang, Meng Wu, Qin Wang, Lusong Luo, Haikuo Ma, Xiaohu Zhang & Sudan He. (2018) Discovery of a potent hedgehog pathway inhibitor capable of activating caspase8-dependent apoptosis. Journal of Pharmacological Sciences 137:3, pages 256-264.
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Chenglin Wang, Mingfei Zhu, Xiuhong Lu, Hong Wang, Weili Zhao, Xiongwen Zhang & Xiaochun Dong. (2018) Synthesis and evaluation of novel dimethylpyridazine derivatives as hedgehog signaling pathway inhibitors. Bioorganic & Medicinal Chemistry 26:12, pages 3308-3320.
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Minhang Xin, Xinyue Ji, Ladie Kimberly De La Cruz, Suresh Thareja & Binghe Wang. (2018) Strategies to target the Hedgehog signaling pathway for cancer therapy. Medicinal Research Reviews 38:3, pages 870-913.
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Wenlu Li, Qinsheng Sun, Lu Song, Chunmei Gao, Feng Liu, Yuzong Chen & Yuyang Jiang. (2017) Discovery of 1-(3-aryl-4-chlorophenyl)-3-( p -aryl)urea derivatives against breast cancer by inhibiting PI3K/Akt/mTOR and Hedgehog signalings. European Journal of Medicinal Chemistry 141, pages 721-733.
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Wenfeng Lu, Yongqiang Liu, Haikuo Ma, Jiyue Zheng, Sheng Tian, Zhijian Sun, Lusong Luo, Jiajun Li, Hongjian Zhang, Zeng-Jie Yang & Xiaohu Zhang. (2017) Design, Synthesis, and Structure–Activity Relationship of Tetrahydropyrido[4,3- d ]pyrimidine Derivatives as Potent Smoothened Antagonists with in Vivo Activity . ACS Chemical Neuroscience 8:9, pages 1980-1994.
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Xiuhong Lu, Yuanqiu Peng, Chenglin Wang, Jun Yang, Xiaolong Bao, Qian Dong, Weili Zhao, Wenfu Tan & Xiaochun Dong. (2017) Design, synthesis, and biological evaluation of optimized phthalazine derivatives as hedgehog signaling pathway inhibitors. European Journal of Medicinal Chemistry 138, pages 384-395.
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Deepak Bhattarai, Joo Hyun Jung, Seunghyeon Han, Hankyu Lee, Soo Jin Oh, Hyuk Wan Ko & Kyeong Lee. (2017) Design, synthesis, and biological evaluation of structurally modified isoindolinone and quinazolinone derivatives as hedgehog pathway inhibitors. European Journal of Medicinal Chemistry 125, pages 1036-1050.
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Daniel Coluccia, Adrienne Weeks, Javier Fandino, Christian Schneider, Christian Smith & James T. Rutka. 2017. The Molecular Basis of Human Cancer. The Molecular Basis of Human Cancer 657 694 .
Xiaolong Bao, Yuanqiu Peng, Xiuhong Lu, Jun Yang, Weili Zhao, Wenfu Tan & Xiaochun Dong. (2016) Synthesis and evaluation of novel benzylphthalazine derivatives as hedgehog signaling pathway inhibitors. Bioorganic & Medicinal Chemistry Letters 26:13, pages 3048-3051.
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Emilie Lauressergues, Peter Heusler, Fabrice Lestienne, David Troulier, Isabelle Rauly‐Lestienne, Amélie Tourette, Marie‐Christine Ailhaud, Claudie Cathala, Stéphanie Tardif, Delphine Denais‐Laliève, Marie‐Thérèse Calmettes, Anne‐Dominique Degryse, Antoine Dumoulin, Luc De Vries & Didier Cussac. (2016) Pharmacological evaluation of a series of smoothened antagonists in signaling pathways and after topical application in a depilated mouse model. Pharmacology Research & Perspectives 4:2.
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Audrey Fleury, Lucile Hoch, M. Carmen Martinez, Hélène Faure, Maurizio Taddei, Elena Petricci, Fabrizio Manetti, Nicolas Girard, André Mann, Caroline Jacques, Jérôme Larghero, Martial Ruat, Ramaroson Andriantsitohaina & Soazig Le Lay. (2016) Hedgehog associated to microparticles inhibits adipocyte differentiation via a non-canonical pathway. Scientific Reports 6:1.
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Monica Benvenuto, Laura Masuelli, Enrico De Smaele, Massimo Fantini, Rosanna Mattera, Danilo Cucchi, Elena Bonanno, Enrica Di Stefano, Giovanni Vanni Frajese, Augusto Orlandi, Isabella Screpanti, Alberto Gulino, Andrea Modesti & Roberto Bei. (2016) In vitro and in vivo inhibition of breast cancer cell growth by targeting the Hedgehog/GLI pathway with SMO (GDC-0449) or GLI (GANT-61) inhibitors . Oncotarget 7:8, pages 9250-9270.
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Chi-Yu Sun, Yang-Sheng Li, Ai-Long Shi, Ya-Fei Li, Rui-Fang Cao, Huai-Wei Ding, Qing-Qing Yin, Li-Juan Zhang, Hua-Chuan Zheng & Hong-Rui Song. (2015) Synthesis and antiproliferative activity of novel 4-substituted-phenoxy-benzamide derivatives. Chinese Chemical Letters 26:10, pages 1307-1310.
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Stacey Ward & Joshua Rubin. (2015) Not so Fast: Co-Requirements for Sonic Hedgehog Induced Brain Tumorigenesis. Cancers 7:3, pages 1484-1498.
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Paola Infante, Romina Alfonsi, Bruno Botta, Mattia Mori & Lucia Di Marcotullio. (2015) Targeting GLI factors to inhibit the Hedgehog pathway. Trends in Pharmacological Sciences 36:8, pages 547-558.
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Ram Kumar & Bruno Fuchs. (2015) Hedgehog Signaling Inhibitors as Anti-Cancer Agents in Osteosarcoma. Cancers 7:2, pages 784-794.
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Lucile Hoch, Helene Faure, Hermine Roudaut, Angele Schoenfelder, Andre Mann, Nicolas Girard, Laure Bihannic, Olivier Ayrault, Elena Petricci, Maurizio Taddei, Didier Rognan & Martial Ruat. (2015) MRT‐92 inhibits Hedgehog signaling by blocking overlapping binding sites in the transmembrane domain of the Smoothened receptor. The FASEB Journal 29:5, pages 1817-1829.
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Isabella FincoChristopher R. LaPenseeKenneth T. KrillGary D. Hammer. (2015) Hedgehog Signaling and Steroidogenesis. Annual Review of Physiology 77:1, pages 105-129.
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Chiyu Sun, Yangsheng Li, Ailong Shi, Jingzhou Zhang, Yafei Li, Mingming Zhao, Lijuan Zhang, Huachuan Zheng, Ying Meng, Huaiwei Ding & Hongrui Song. (2015) Synthesis and evaluation of novel N-3-benzimidazolephenylbisamide derivatives for antiproliferative and Hedgehog pathway inhibitory activity. MedChemComm 6:6, pages 1137-1142.
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Haikuo Ma, Wenfeng Lu, Zhijian Sun, Lusong Luo, Delong Geng, Zhaohui Yang, Enqin Li, Jiyue Zheng, Meiyu Wang, Hongjian Zhang, Shilin Yang & Xiaohu Zhang. (2015) Design, synthesis, and structure–activity-relationship of tetrahydrothiazolopyridine derivatives as potent smoothened antagonists. European Journal of Medicinal Chemistry 89, pages 721-732.
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Martial Ruat & Lucile Hoch. 2015. The Smoothened Receptor in Cancer and Regenerative Medicine. The Smoothened Receptor in Cancer and Regenerative Medicine 1 11 .
Liandi Zhang, Minhang Xin, Han Shen, Jun Wen, Feng Tang, Chongxing Tu, Xinge Zhao & Ping Wei. (2014) Five-membered heteroaromatic ring fused-pyrimidine derivatives: Design, synthesis, and hedgehog signaling pathway inhibition study. Bioorganic & Medicinal Chemistry Letters 24:15, pages 3486-3492.
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Minhang Xin, Liandi Zhang, Han Shen, Jun Wen, Chongxing Tu, Zhaoyu Liu, Lingfei Cheng & Xinge Zhao. (2014) Design, synthesis, and biological study of 6,7-dihydro-5H-pyrano[2,3-d]pyrimidine derivatives as novel hedgehog signaling pathway inhibitors. Medicinal Chemistry Research 23:8, pages 3784-3792.
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Albert M. DeBerardinis, Daniel J. Madden, Upasana Banerjee, Vibhavari Sail, Daniel S. Raccuia, Daniel De Carlo, Steven M. Lemieux, Adam Meares & M. Kyle Hadden. (2014) Structure–Activity Relationships for Vitamin D3-Based Aromatic A-Ring Analogues as Hedgehog Pathway Inhibitors. Journal of Medicinal Chemistry 57:9, pages 3724-3736.
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Wenfeng Lu, Delong Geng, Zhijian Sun, Zhaohui Yang, Haikuo Ma, Jiyue Zheng & Xiaohu Zhang. (2014) Scaffold hopping approach to a new series of smoothened antagonists. Bioorganic & Medicinal Chemistry Letters 24:10, pages 2300-2304.
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Juanita L. Merchant & Milena Saqui-Salces. (2014) Inhibition of Hedgehog signaling in the gastrointestinal tract: Targeting the cancer microenvironment. Cancer Treatment Reviews 40:1, pages 12-21.
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Minhang Xin, Jun Wen, Feng Tang, Chongxing Tu, Wei Huang, Han Shen, Xinge Zhao, Lingfei Cheng, Mengyu Wang & Liandi Zhang. (2014) Synthesis and evaluation of 4-(2-pyrimidinylamino) benzamides inhibitors of hedgehog signaling pathway. Bioorganic & Medicinal Chemistry Letters 24:3, pages 983-988.
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Minhang Xin, Liandi Zhang, Feng Tang, Chongxing Tu, Jun Wen, Xinge Zhao, Zhaoyu Liu, Lingfei Cheng & Han Shen. (2014) Design, synthesis, and evaluation of pyrrolo[2,1-f][1,2,4]triazine derivatives as novel hedgehog signaling pathway inhibitors. Bioorganic & Medicinal Chemistry 22:4, pages 1429-1440.
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Trieu N. Trinh, Lacey Hizartzidis, Andrew J. S. Lin, David G. Harman, Adam McCluskey & Christopher P. Gordon. (2014) An efficient continuous flow approach to furnish furan-based biaryls. Org. Biomol. Chem. 12:47, pages 9562-9571.
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Arokia Priyanka Vaz, Parthasarathy Seshacharyulu, Surinder K. Batra & Moorthy P. Ponnusamy. 2014. Stem Cells and Cancer Stem Cells, Volume 11. Stem Cells and Cancer Stem Cells, Volume 11 171 185 .
Martial Ruat, Hélène Faure & Mathieu Daynac. 2015. The Smoothened Receptor in Cancer and Regenerative Medicine. The Smoothened Receptor in Cancer and Regenerative Medicine 147 171 .
Martial Ruat, Lucile Hoch, Hélène Faure & Didier Rognan. (2013) Structure du récepteur Smoothened. médecine/sciences 29:10, pages 855-860.
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