Zobrazeno 1 - 10
of 64
pro vyhledávání: '"Jingwu Duan"'
Autor:
Mian Gao, David J. Shuster, Hai-Yun Xiao, Christine B. Goldstine, Jing Chen, Zhonghui Lu, Victor R. Guarino, Khehyong Ngu, Lisa M. Kopcho, Deepa Calambur, Kurt R. Gregor, Andrew J. Tebben, Jingwu Duan, Luisa Salter-Cid, Hao Lu, Joseph A. Tino, Ning Li, John Hynes, James R. Burke, Joseph Yanchunas, John E. Macor, Steven Sheriff, Dauh-Rurng Wu, Bin Jiang, Patrick J. Shaw, ChiehYing Y. Chang, Jenny Xie, Vojkan Susulic, T. G. Murali Dhar
Publikováno v:
Journal of Medicinal Chemistry. 63:15050-15071
Scaffold hopping and structure-based drug design were employed to identify substituted 4-aminoquinolines and 4-aminonaphthyridines as potent, small molecule inhibitors of tumor necrosis factor alpha (TNFα). Structure-activity relationships in both t
Autor:
Carolyn A. Weigelt, Sha Li, David Marcoux, Georgia Cornelius, Qihong Zhao, Mary Ellen Cvijic, John E. Macor, Jingwu Duan, Melissa Yarde, Muthalagu Vetrichelvan, David J. Shuster, Qingjie Liu, Richard Rampulla, Kim W. McIntyre, Mary T. Obermeier, Shiuhang Yip, Purnima Khandelwal, Sureshbabu Vishwakrishnan, Anuradha Gupta, Virna Borowski, Peng Li, Kevin Stefanski, Sridharan Ramlingam, Myra Beaudoin-Bertrand, Nageswara Maddala, Sridhar Vanteru, Percy H. Carter, Arvind Mathur, Aberra Fura, Max Ruzanov, John Hynes, Dauh-Rurng Wu, Jinhong Wang, Luisa Salter-Cid, John S. Sack, Cornelius Lyndon A M, Anurag S. Srivastava, Robert J. Cherney, Kumaravel Selvakumar, Mushkin Basha, Arun Kumar Gupta, Douglas G. Batt, Rex Denton, Sukhen Karmakar, Qing Shi, Ananta Karmakar, Naveen Manjunath, Javed Khan, Jenny Xie, Joseph A. Tino, T. G. Murali Dhar
Publikováno v:
Journal of Medicinal Chemistry. 62:9931-9946
RORγt is an important nuclear receptor that regulates the production of several pro-inflammatory cytokines such as IL-17 and IL-22. As a result, RORγt has been identified as a potential target for the treatment of various immunological disorders su
Autor:
Bin Jiang, Sylwia Stachura, T. G. Murali Dhar, Carolyn A. Weigelt, Dauh Rurng Wu, Jingwu Duan, Luisa M. Salter–Cid, Javed Khan, Ding Ren Shen, Melissa Yarde, Qihong Zhao, Zhonghui Lu, Percy H. Carter, John S. Sack, Max Ruzanov
Publikováno v:
Bioorganicmedicinal chemistry letters. 30(19)
In an effort to discover oral inverse agonists of RORγt to treat inflammatory diseases, a new 2,6–difluorobenzyl ether series of cyclopentyl sulfones were found to be surprisingly more potent than the corresponding alcohol derivatives. When combin
Autor:
Yanling Huang, Jingwu Duan, Carolyn A. Weigelt, Cullen L. Cavallaro, Javed Khan, Brian E. Fink, Muthoni G. Kamau, Zheming Ruan, Lan-Ying Qin, Sylwia Stachura, Cliff Chen, Murali Gururajan, Lalgudi S. Harikrishnan, Tram N. Huynh, John S. Sack, Anwar Murtaza, Daniel O'malley, Zhuyin Li, Melissa Yarde, Max Ruzanov, Virna Borowski, Patrice Gill, Huadong Sun, Zhonghui Lu, Jessica J. Wong
Publikováno v:
Bioorganicmedicinal chemistry letters. 30(12)
Substituted benzyloxy aryl compound 2 was identified as an RORγt agonist. Structure based drug design efforts resulted in a potent and selective tricyclic compound 19 which, when administered orally in an MC38 mouse tumor model, demonstrated a desir
Autor:
Qingjie Liu, Mary T. Obermeier, John S. Sack, Carolyn A. Weigelt, Georgia Cornelius, Percy H. Carter, David J. Shuster, Luisa Salter-Cid, Aberra Fura, Virna Borowski, Jingwu Duan, Purnima Khandelwal, Qing Shi, Robert J. Cherney, Cornelius Lyndon A M, Jinhong Wang, Jenny Xie, Max Ruzanov, Kevin Stefanski, Rex Denton, T. G. Murali Dhar, David Marcoux, Shiuhang Yip, Melissa Yarde, Douglas G. Batt, Javed Khan, Joseph A. Tino, Qihong Zhao, Anurag S. Srivastava, Arvind Mathur, Mary Ellen Cvijic, John E. Macor, Sha Li, Dauh-Rurng Wu
Publikováno v:
ACS Med Chem Lett
[Image: see text] Novel tricyclic analogues were designed, synthesized, and evaluated as RORγt inverse agonists. Several of these compounds were potent in an IL-17 human whole blood assay and exhibited excellent oral bioavailability in mouse pharmac
Autor:
Celia D’Arienzo, Ananta Karmakar, Marta Dabros, Michael Galella, Jingwu Duan, John S. Sack, Dhanya Kumar Raut, David S. Weinstein, Andrew T. Pudzianowski, Ding-Ren Shen, Sylwia Stachura, Joel C. Barrish, Arun Kumar Gupta, Huadong Sun, William R. Foster, Javed Khan, Melissa Yarde, Dan Camac, Lauren Haque, Qihong Zhao, Dauh-Rurng Wu, Carolyn A. Weigelt, Faye Wang, Percy H. Carter, Luisa Salter-Cid, Hemalatha Hemagiri, Jenny Xie, T. G. Murali Dhar, Zhonghui Lu, Virna Borowski, Hua Gong, John E. Somerville
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:85-93
We disclose the optimization of a high throughput screening hit to yield benzothiazine and tetrahydroquinoline sulfonamides as potent RORγt inverse agonists. However, a majority of these compounds showed potent activity against pregnane X receptor (
Autor:
John S. Sack, Sylwia Stachura, Bin Jiang, Sridhar Vanteru, Percy H. Carter, Lisa Zhang, Max Ruzanov, Javed Khan, Zhonghui Lu, Jenny Xie, Jingwu Duan, Qihong Zhao, Ding-Ren Shen, Luisa Salter-Cid, T. G. Murali Dhar, Dauh-Rurng Wu, Arvind Mathur, David J. Shuster, Virna Borowski, Arun Kumar Gupta, Carolyn A. Weigelt, Michael Galella, William R. Foster, Melissa Yarde
[Image: see text] A new phenyl (3-phenylpyrrolidin-3-yl)sulfone series of RORγt inverse agonists was discovered utilizing the binding conformation of previously reported bicyclic sulfonamide 1. Through a combination of structure-based design and str
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::291851fb8201f5b23025040c19f28f3e
https://europepmc.org/articles/PMC6421587/
https://europepmc.org/articles/PMC6421587/
Autor:
Javed Khan, Dhanya Kumar Raut, Sylwia Stachura, Qihong Zhao, Jingwu Duan, Melissa Yarde, Bin Jiang, Hemalatha Hemagiri, Arvind Mathur, Ananta Karmakar, Michael Galella, T. G. Murali Dhar, John S. Sack, Percy H. Carter, Luisa Salter-Cid, Arun Kumar Gupta, Carolyn A. Weigelt, Dauh-Rurng Wu, Ding-Ren Shen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 30:127392
A novel series of cis-3,4-diphenylpyrrolidines were designed as RORγt inverse agonists based on the binding conformation of previously reported bicyclic sulfonamide 1. Preliminary synthesis and structure–activity relationship (SAR) study establish
Autor:
Jingwu Duan, Hai-Yun Xiao, Steven G. Nadler, Kim W. McIntyre, Michael Galella, Bin Jiang, Zili Xiao, Julie Carman, Sium Habte, Luisa Salter-Cid, Mark D. Cunningham, T.G. Dhar, Deborah A. Holloway, Jinhong Wang, David J. Shuster, John E. Somerville, David S. Weinstein, Michael G. Yang, Joel C. Barrish
Publikováno v:
Journal of Medicinal Chemistry. 58:4278-4290
An empirical approach to improve the microsomal stability and CYP inhibition profile of lead compounds 1a and 1b led to the identification of 5 (BMS-341) as a dissociated glucocorticoid receptor modulator. Compound 5 showed significant improvements i
Autor:
Joel C. Barrish, Aberra Fura, Guoxiang Shen, Jingwu Duan, David S. Nirschl, Jonathan Lippy, Stephen T. Wrobleski, Rosemary Zhang, Lidia M. Doweyko, Bingwei V. Yang, Lauren Haque, Murray McKinnon, Shuqun Lin, Luisa Salter-Cid, Sidney Pitt, William J. Pitts, Percy H. Carter, John S. Sack, Gary L. Schieven, Bin Jiang, John Hynes, Gregory D. Brown, John S. Tokarski, Zhonghui Lu, Javed Khan, Steven G. Nadler
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:5721-5726
A new class of Janus kinase (JAK) inhibitors was discovered using a rationally designed pyrrolo[1,2-b]pyridazine-3-carboxamide scaffold. Preliminary studies identified (R)-(2,2-dimethylcyclopentyl)amine as a preferred C4 substituent on the pyrrolopyr