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Recent advances in the development of novel glucocorticoid receptor modulators

Pages 855-873 | Published online: 16 Jun 2010

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Yuan Liang, Qiuyan Jiang, Haoyang Zou, Jingqi Zhao, Jie Zhang & Li Ren. (2023) Withaferin A: A potential selective glucocorticoid receptor modulator with anti-inflammatory effect. Food and Chemical Toxicology 179, pages 113949.
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Amy Han, Olav Olsen, Christopher D’Souza, Jing Shan, Feng Zhao, Jean Yanolatos, Zaruhi Hovhannisyan, Sokol Haxhinasto, Frank Delfino & William Olson. (2021) Development of Novel Glucocorticoids for Use in Antibody–Drug Conjugates for the Treatment of Inflammatory Diseases. Journal of Medicinal Chemistry 64:16, pages 11958-11971.
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Mohamed A. Morsy, Snehal S. Patel, Azza A. K. El-Sheikh, Jignasa K. Savjani, Anroop B. Nair, Jigar N. Shah & Katharigatta N. Venugopala. (2019) Computational and Biological Comparisons of Plant Steroids as Modulators of Inflammation through Interacting with Glucocorticoid Receptor. Mediators of Inflammation 2019, pages 1-9.
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Olga Savvidou, Mandy Milonaki, Stavros Goumenos, Dimitrios Flevas, Panayiotis Papagelopoulos & Paraskevi Moutsatsou. (2019) Glucocorticoid signaling and osteoarthritis. Molecular and Cellular Endocrinology 480, pages 153-166.
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Hiromasa Yoshioka, Ayumi Yamada, Yuko Nishiyama, Hiroyuki Kagechika, Yuichi Hashimoto & Shinya Fujii. (2017) Development of nonsteroidal glucocorticoid receptor modulators based on N-benzyl-N-(4-phenoxyphenyl)benzenesulfonamide scaffold. Bioorganic & Medicinal Chemistry 25:13, pages 3461-3470.
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Markus Berger, Hartmut Rehwinkel, Norbert Schmees, Heike Schäcke, Karl Edman, Lisa Wissler, Andreas Reichel & Stefan Jaroch. (2017) Discovery of new selective glucocorticoid receptor agonist leads. Bioorganic & Medicinal Chemistry Letters 27:3, pages 437-442.
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Dona L. Fleishaker, Arnab Mukherjee, Fredrick S. Whaley, Shanthini Daniel & Bernhardt G. Zeiher. (2016) Safety and pharmacodynamic dose response of short-term prednisone in healthy adult subjects: a dose ranging, randomized, placebo-controlled, crossover study. BMC Musculoskeletal Disorders 17:1.
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Christel A.S. Bergström, William N. Charman & Christopher J.H. Porter. (2016) Computational prediction of formulation strategies for beyond-rule-of-5 compounds. Advanced Drug Delivery Reviews 101, pages 6-21.
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Bachir Latli, Jonathan T. Reeves, Zhulin Tan, Matt Hrapchak, Jinhua J. Song, Carl B. Busacca & Chris H. Senanayake. (2015) Synthesis of two potent glucocorticoid receptor agonists labeled with carbon-14 and stable isotopes. Journal of Labelled Compounds and Radiopharmaceuticals 58:11-12, pages 445-452.
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Michael G. Yang, T. G. Murali Dhar, Zili Xiao, Hai-Yun Xiao, James J.-W. Duan, Bin Jiang, Michael A. Galella, Mark Cunningham, Jinhong Wang, Sium Habte, David Shuster, Kim W. McIntyre, Julie Carman, Deborah A. Holloway, John E. Somerville, Steven G. Nadler, Luisa Salter-Cid, Joel C. Barrish & David S. Weinstein. (2015) Improving the Pharmacokinetic and CYP Inhibition Profiles of Azaxanthene-Based Glucocorticoid Receptor Modulators—Identification of ( S )-5-(2-(9-Fluoro-2-(4-(2-hydroxypropan-2-yl)phenyl)-5 H -chromeno[2,3- b ]pyridin-5-yl)-2-methylpropanamido)- N -(tetrahydro-2 H -pyran-4-yl)-1,3,4-thiadiazole-2-carboxamide (BMS-341) . Journal of Medicinal Chemistry 58:10, pages 4278-4290.
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Clemens Honeder, Elisabeth Engleder, Hanna Schöpper, Markus Krause, Lukas David Landegger, Roberto Plasenzotti, Franz Gabor, Wolfgang Gstoettner & Christoph Arnoldner. (2014) Evaluation of the selective glucocorticoid receptor agonist compound A for ototoxic effects . The Laryngoscope 125:4.
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Yves A. Chantigny, John C. Murray, Edward F. Kleinman, Ralph P. Robinson, Michael A. Plotkin, Matthew R. Reese, Leonard Buckbinder, Patricia A. McNiff, Michele L. Millham, Jean F. Schaefer, Yuriy A. Abramov & Jon Bordner. (2015) 2-Aryl-3-methyloctahydrophenanthrene-2,3,7-triols as Potent Dissociated Glucocorticoid Receptor Agonists. Journal of Medicinal Chemistry 58:6, pages 2658-2677.
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Christian Harcken, Doris Riether, Pingrong Liu, Hossein Razavi, Usha Patel, Thomas Lee, Todd Bosanac, Yancey Ward, Mark Ralph, Zhidong Chen, Donald Souza, Richard M. Nelson, Alison Kukulka, Tazmeen N. Fadra-Khan, Ljiljana Zuvela-Jelaska, Mita Patel, David S. Thomson & Gerald H. Nabozny. (2014) Optimization of Drug-Like Properties of Nonsteroidal Glucocorticoid Mimetics and Identification of a Clinical Candidate. ACS Medicinal Chemistry Letters 5:12, pages 1318-1323.
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Richard P. Loach, Owen S. Fenton, Kazuma Amaike, Dustin S. Siegel, Erhan Ozkal & Mohammad Movassaghi. (2014) C7-Derivatization of C3-Alkylindoles Including Tryptophans and Tryptamines. The Journal of Organic Chemistry 79:22, pages 11254-11263.
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Sulur G. Manjunatha, Sreekanth Bachu, Vasantha Krishna Kadambar, Andiappan Murugan, Sridharan Ramasubramanian, Puranik Ramachandra & Sudhir Nambiar. (2014) A novel synthetic approach to 4-acetamido-1-arylindazoles via Semmler?Wolff rearrangement of 1-aryl-6,7-dihydro-5H-indazol-4-one oxime. Tetrahedron Letters 55:22, pages 3348-3350.
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Hossein Razavi, Doris Riether, Christian Harcken, Jörg Bentzien, Roger M. Dinallo, Donald Souza, Richard M. Nelson, Alison Kukulka, Tazmeen N. Fadra-Khan, Edward J. PackJr.Jr., Ljiljana Zuvela-Jelaska, Josephine Pelletier, Mark Panzenbeck, Carol A. Torcellini, John R. Proudfoot, Gerald H. Nabozny & David S. Thomson. (2014) Discovery of a potent and dissociated non-steroidal glucocorticoid receptor agonist containing an alkyl carbinol pharmacophore. Bioorganic & Medicinal Chemistry Letters 24:8, pages 1934-1940.
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Christian Harcken, Doris Riether, Daniel Kuzmich, Pingrong Liu, Raj Betageri, Mark Ralph, Michel Emmanuel, Jonathan T. Reeves, Angela Berry, Donald Souza, Richard M. Nelson, Alison Kukulka, Tazmeen N. Fadra, Ljiljana Zuvela-Jelaska, Roger Dinallo, Jörg Bentzien, Gerald H. Nabozny & David S. Thomson. (2014) Identification of Highly Efficacious Glucocorticoid Receptor Agonists with a Potential for Reduced Clinical Bone Side Effects. Journal of Medicinal Chemistry 57:4, pages 1583-1598.
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Philip E. Brandish, Kenneth Anderson, Gretchen A. Baltus, Chang Bai, Christopher J. Bungard, Patricia Bunting, Alan Byford, Chi-Sung Chiu, Milenko Cicmil, Halea Corcoran, Danielle Euler, John E. Fisher, Carlo Gambone, Martha Hasbun-Manning, Nelly Kuklin, Elizabeth Landis, Traci Q. Lifsted, Sheila McElwee-Witmer, Ian S. McIntosh, Robert S. Meissner, John Miao, Helen J. Mitchell, Amy Musselman, Azriel Schmidt, John Shin, Peter Szczerba, Charles D. Thompson, Catherine Tribouley, Robert L. Vogel, Sudha Warrier & James C. Hershey. (2014) The preclinical efficacy, selectivity and pharmacologic profile of MK-5932, an insulin-sparing selective glucocorticoid receptor modulator. European Journal of Pharmacology 724, pages 102-111.
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Hai-Yun Xiao, Dauh-Rurng Wu, James E. SheppeckIIII, Sium F. Habte, Mark D. Cunningham, John E. Somerville, Joel C. Barrish, Steven G. Nadler & T.G. Murali Dhar. (2013) Heterocyclic glucocorticoid receptor modulators with a 2,2-dimethyl-3-phenyl-N-(thiazol or thiadiazol-2-yl)propanamide core. Bioorganic & Medicinal Chemistry Letters 23:20, pages 5571-5574.
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Xue-Yuan Chen, Shan-Mei Wang, Nan Li, Yang Hu, Yuan Zhang, Jin-Fu Xu, Xia Li, Jie Ren, Bo Su, Wei-Zhong Yuan, Xin-Rong Teng, Rong-Xuan Zhang, Dian-hua Jiang, Xavier Mulet & Hui-Ping Li. (2013) Creation of Lung-Targeted Dexamethasone Immunoliposome and Its Therapeutic Effect on Bleomycin-Induced Lung Injury in Rats. PLoS ONE 8:3, pages e58275.
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Andrew R. Clark & Maria G. Belvisi. (2012) Maps and legends: The quest for dissociated ligands of the glucocorticoid receptor. Pharmacology & Therapeutics 134:1, pages 54-67.
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Eugénie Joanny, Qize Ding, Leyi Gong, Philip Kong, Jeremy Saklatvala & Andrew R Clark. (2012) Anti‐inflammatory effects of selective glucocorticoid receptor modulators are partially dependent on up‐regulation of dual specificity phosphatase 1. British Journal of Pharmacology 165:4b, pages 1124-1136.
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Raj Betageri, Thomas Gilmore, Daniel Kuzmich, Thomas M. Kirrane, Jörg Bentzien, Dieter Wiedenmayer, Younes Bekkali, John Regan, Angela Berry, Bachir Latli, Alison J. Kukulka, Tazmeen N. Fadra, Richard M. Nelson, Susan Goldrick, Ljiljana Zuvela-Jelaska, Don Souza, Josephine Pelletier, Roger Dinallo, Mark Panzenbeck, Carol Torcellini, Heewon Lee, Edward Pack, Christian Harcken, Gerald Nabozny & David S. Thomson. (2011) Non-steroidal dissociated glucocorticoid agonists: indoles as A-ring mimetics and function-regulating pharmacophores. Bioorganic & Medicinal Chemistry Letters 21:22, pages 6842-6851.
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David S. Weinstein, Hua Gong, Arthur M. Doweyko, Mark Cunningham, Sium Habte, Jin Hong Wang, Deborah A. Holloway, Christine Burke, Ling Gao, Victor Guarino, Julie Carman, John E. Somerville, David Shuster, Luisa Salter-Cid, John H. Dodd, Steven G. Nadler & Joel C. Barrish. (2011) Azaxanthene Based Selective Glucocorticoid Receptor Modulators: Design, Synthesis, and Pharmacological Evaluation of ( S )-4-(5-(1-((1,3,4-Thiadiazol-2-yl)amino)-2-methyl-1-oxopropan-2-yl)-5 H -chromeno[2,3- b ]pyridin-2-yl)-2-fluoro- N , N -dimethylbenzamide (BMS-776532) and Its Methylene Homologue (BMS-791826) . Journal of Medicinal Chemistry 54:20, pages 7318-7333.
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Masatomo KatoYumi HagiwaraTomoko OdaMiwa Imamura-TakaiHiroyuki AonoMasatsugu Nakamura. (2011) Beneficial Pharmacological Effects of Selective Glucocorticoid Receptor Agonist in External Eye Diseases. Journal of Ocular Pharmacology and Therapeutics 27:4, pages 353-360.
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Neil J. McKenna. (2011) Discovery-driven research and bioinformatics in nuclear receptor and coregulator signaling. Biochimica et Biophysica Acta (BBA) - Molecular Basis of Disease 1812:8, pages 808-817.
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Steven L. Roach, Robert I. Higuchi, Andrew R. Hudson, Angie Vassar, Virginia H.S. Grant, Ryan Lamer, Charlene Hooper, Deepa Rungta, Peter M. Syka, Dale E. Mais, Keith B. Marschke & Lin Zhi. (2011) Tetrahydroquinolin-3-yl carbamate glucocorticoid receptor agonists with reduced PEPCK activation. Bioorganic & Medicinal Chemistry Letters 21:6, pages 1658-1662.
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Takaaki Sumiyoshi, Kengo Tojo, Daisuke Urabe & Masanori Tobe. (2011) Asymmetric synthesis of the 6-cyanoindole derivatives as non-steroidal glucocorticoid receptor modulators using (+)- and (−)-tert-butyl 6-cyano-3-[3-ethoxy-1,1,1-trifluoro-2-hydroxy-3-oxopropan-2-yl]-1H-indole-1-carboxylate. Tetrahedron: Asymmetry 22:2, pages 153-160.
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Bingwei V. Yang, David S. Weinstein, Lidia M. Doweyko, Hua Gong, Wayne Vaccaro, Tram Huynh, Hai-yun Xiao, Arthur M. Doweyko, Lorraine Mckay, Deborah A. Holloway, John E. Somerville, Sium Habte, Mark Cunningham, Michele McMahon, Robert Townsend, David Shuster, John H. Dodd, Steven G. Nadler & Joel C. Barrish. (2010) Dimethyl-diphenyl-propanamide Derivatives As Nonsteroidal Dissociated Glucocorticoid Receptor Agonists. Journal of Medicinal Chemistry 53:23, pages 8241-8251.
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Doris Riether, Christian Harcken, Hossein Razavi, Daniel Kuzmich, Thomas Gilmore, Jörg Bentzien, Edward J. PackJr.Jr., Donald Souza, Richard M. Nelson, Alison Kukulka, Tazmeen N. Fadra, Ljiljana Zuvela-Jelaska, Josephine Pelletier, Roger Dinallo, Mark Panzenbeck, Carol Torcellini, Gerald H. Nabozny & David S. Thomson. (2010) Nonsteroidal Dissociated Glucocorticoid Agonists Containing Azaindoles as Steroid A-Ring Mimetics. Journal of Medicinal Chemistry 53:18, pages 6681-6698.
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