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Recent advances in the design of Hedgehog pathway inhibitors for the treatment of malignancies

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Heng Fong Seow, Wai Kien Yip & Theodora Fifis. (2016) Advances in targeted and immunobased therapies for colorectal cancer in the genomic era. OncoTargets and Therapy 9, pages 1899-1920.
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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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M Kyle Hadden. (2015) Targeting GLI proteins in human cancer by small molecules (WO2014116651 A1): a patent evaluation. Expert Opinion on Therapeutic Patents 25:5, pages 613-617.
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Articles from other publishers (22)

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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Jiachen Wen, Kelly A. Teske & M. Kyle Hadden. (2020) Inhibition of hedgehog signaling by stereochemically defined des-triazole itraconazole analogues. Bioorganic & Medicinal Chemistry Letters 30:2, pages 126794.
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Chiyu Sun, Ying Zhang, Lin Lin, Shuyuan Liu, Rui Wang, Wei Zang, Weijia Meng & Xiaofeng Chen. (2019) Synthesis and Evaluation of Aminothiazole Derivatives as Hedgehog Pathway Inhibitors. Chemistry & Biodiversity 16:12.
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Álvaro Cañete-Molina, Christian Espinosa-Bustos, Marcos González-Castro, Mario Faúndez, Jaime Mella, Ricardo A. Tapia, Alan R. Cabrera, Iván Brito, Adam Aguirre & Cristian O. Salas. (2019) Design, synthesis, cytotoxicity and 3D-QSAR analysis of new 3,6-disubstituted-1,2,4,5-tetrazine derivatives as potential antitumor agents. Arabian Journal of Chemistry 12:7, pages 1092-1107.
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Christian Espinosa-Bustos, Jaime Mella, Jorge Soto-Delgado & Cristian O Salas. (2019) State of the art of Smo antagonists for cancer therapy: advances in the target receptor and new ligand structures. Future Medicinal Chemistry 11:6, pages 617-638.
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Heng Zhang, Zhijun Sun, Zhaopeng Liu & Chun Song. (2018) Overcoming the emerging drug resistance of smoothened: an overview of small-molecule SMO antagonists with antiresistance activity. Future Medicinal Chemistry 10:24, pages 2855-2875.
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Minhang Xin, Liandi Zhang, Chongxing Tu, Feng Tang & Jun Wen. (2018) Novel 4-(2-pyrimidinylamino)benzamide derivatives as potent hedgehog signaling pathway inhibitors. Bioorganic & Medicinal Chemistry 26:18, pages 5029-5036.
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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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Y. Wang, P. Lu, D. Zhao & J. Sheng. (2016) Targeting the hedgehog signaling pathway for cardiac repair and regenerationDer Hedgehog-Signalweg als Zielpunkt bei kardialer Wiederherstellung und Regeneration. Herz 42:7, pages 662-668.
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Chad A. Maschinot & M. Kyle Hadden. (2017) Synthesis and evaluation of vitamin D3 analogues with C-11 modifications as inhibitors of Hedgehog signaling. Bioorganic & Medicinal Chemistry Letters 27:17, pages 4011-4014.
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Minhang Xin, Liandi Zhang, Jun Wen, Han Shen, Xinge Zhao, Qiu Jin & Feng Tang. (2017) Introduction of fluorine to phenyl group of 4-(2-pyrimidinylamino)benzamides leading to a series of potent hedgehog signaling pathway inhibitors. Bioorganic & Medicinal Chemistry Letters 27:15, pages 3259-3263.
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Mingliang Guo, Kwon Ho Hong, Yongfeng Lv, Yu Ding, Congcong Li, Hua Xu, Wenxiu Qi, Junqing Chen, Min Ji & Jin Cai. (2019) A Novel and Efficient Route for Synthesis of Taladegib. Journal of Chemical Research 41:2, pages 112-115.
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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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Ju Chen, Haining Lv, Jinping Hu, Ming Ji, Nina Xue, Chao Li, Shuanggang Ma, Qin Zhou, Bin Lin, Yan Li, Shishan Yu & Xiaoguang Chen. (2016) CAT3, a novel agent for medulloblastoma and glioblastoma treatment, inhibits tumor growth by disrupting the Hedgehog signaling pathway. Cancer Letters 381:2, pages 391-403.
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Jennifer R. Pace, Albert M. DeBerardinis, Vibhavari Sail, Silvia K. Tacheva-Grigorova, Kelly A. Chan, Raymond Tran, Daniel S. Raccuia, Robert J. Wechsler-Reya & M. Kyle Hadden. (2016) Repurposing the Clinically Efficacious Antifungal Agent Itraconazole as an Anticancer Chemotherapeutic. Journal of Medicinal Chemistry 59:8, pages 3635-3649.
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Minhang Xin, Liandi Zhang, Qiu Jin, Feng Tang, Jun Wen, Liyun Gu, Lingfei Cheng & Yong Zhao. (2016) Discovery of novel 4-(2-pyrimidinylamino)benzamide derivatives as highly potent and orally available hedgehog signaling pathway inhibitors. European Journal of Medicinal Chemistry 110, pages 115-125.
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Minhang Xin, Liandi Zhang, Jun Wen, Han Shen, Zhaoyu Liu, Xinge Zhao, Qiu Jin, Mengyu Wang, Lingfei Cheng, Wei Huang & Feng Tang. (2016) Synthesis and pharmacological evaluation of trifluoromethyl containing 4-(2-pyrimidinylamino)benzamides as Hedgehog signaling pathway inhibitors. Bioorganic & Medicinal Chemistry 24:5, pages 1079-1088.
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A. Antoniou, M. Chatzopoulou, M. Bantzi, C. M. Athanassopoulos, A. Giannis & E. N. Pitsinos. (2016) Identification of Gli-mediated transcription inhibitors through synthesis and evaluation of taepeenin D analogues. MedChemComm 7:12, pages 2328-2331.
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Xiaofeng Chen, Chiyu Sun, Jingzhou Zhang, Huaiwei Ding & Hongrui Song. (2016) Design, synthesis and evaluation of novel tetrahydrothieno[3,2-c]pyridine derivatives as potent smoothened antagonists. MedChemComm 7:5, pages 960-965.
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ASHLEY L. SPANN, KUN YUAN, KAYLA F. GOLIWAS, ADAM D. STEG, DEVANSHU D. KAUSHIK, YEON-JIN KWON & ANDRA R. FROST. (2015) The presence of primary cilia in cancer cells does not predict responsiveness to modulation of smoothened activity. International Journal of Oncology 47:1, pages 269-279.
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Albert M. DeBerardinis, Daniel S. Raccuia, Evrett N. Thompson, Chad A. Maschinot & M. Kyle Hadden. (2015) Vitamin D3 analogues that contain modified A- and seco-B-rings as hedgehog pathway inhibitors. European Journal of Medicinal Chemistry 93, pages 156-171.
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Upasana Banerjee, Albert M. DeBerardinis & M. Kyle Hadden. (2015) Design, synthesis, and evaluation of hybrid vitamin D3 side chain analogues as hedgehog pathway inhibitors. Bioorganic & Medicinal Chemistry 23:3, pages 548-555.
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