Zobrazeno 1 - 10
of 33
pro vyhledávání: '"Sidney Pitt"'
Autor:
Sidney Pitt, John S. Sack, Vicky Tang, William J. Pitts, Steven H. Spergel, Jonathan Lippy, Junqing Guo, Michael Galella, Mertzman Michael E, Sylwia Stachura, Steven G. Nadler, Aberra Fura, Percy H. Carter, Gary L. Schieven, Luisa Salter-Cid, Kim W. McIntyre, James Kempson, Javed Khan, Lauren Haque, Rosemary Zhang, John S. Tokarski, Guoxiang Shen, Kathleen M. Gillooly, Stephen T. Wrobleski, Joel C. Barrish
[Image: see text] The four members of the Janus family of nonreceptor tyrosine kinases play a significant role in immune function. The JAK family kinase inhibitor, tofacitinib 1, has been approved in the United States for use in rheumatoid arthritis
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ee1a959ab8edd802fd477e946d59e0fb
https://europepmc.org/articles/PMC6421541/
https://europepmc.org/articles/PMC6421541/
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fb7f63858a17538ff6a98f0ae52d3f8e
https://doi.org/10.1016/j.bmcl.2014.10.061
https://doi.org/10.1016/j.bmcl.2014.10.061
Autor:
Dezhi Xing, Carolyn A. Weigelt, Luisa Salter-Cid, Pirama Nayagam Arunachalam, Rodney B.W. Smith, Ling Li, Melissa Yarde, Jodi K. Muckelbauer, Jonathan Lippy, Mary Ellen Cvijic, Sidney Pitt, John S. Sack, Thatipamula Rp, Michael A. Poss, Paul Levesque, Robert J. Cherney, Ipsit Kundu, David Marcoux, Gary L. Schieven, Arvind Mathur, Qingjie Liu, Zheming Ruan, Rosemary Zhang, R M Fancher, Shweta Padmanabhan, Scott H. Watterson, Qing Shi, Mary T. Obermeier, Anurag S. Srivastava, Anuradha Gupta, Douglas G. Batt, James Neels, Joseph A. Tino, Kevin Stefanski, Percy H. Carter, Macor John E, John Hynes, Myra Beaudoin-Bertrand, Hao Lu, Kim W. McIntyre, Stacey Skala, Aberra Fura, Lan-Ying Qin, Cornelius Lyndon A M, James Hennan, Richard Rampulla, Bogdan Sleczka, Jenny Xie, Kallem Rajareddy, Jie Pan, Christine B. Goldstine, Hua Gong, Qian Ruan, Kathleen M. Gillooly, Donna L. Pedicord, Jingsong Fan, Rajeev S. Bhide, Stefan Ruepp
Publikováno v:
Journal of medicinal chemistry. 60(12)
PI3Kδ plays an important role controlling immune cell function and has therefore been identified as a potential target for the treatment of immunological disorders. This article highlights our work toward the identification of a potent, selective, a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e67ea5386a71d40a3c8aca591866f2ab
https://pubmed.ncbi.nlm.nih.gov/28541707
https://pubmed.ncbi.nlm.nih.gov/28541707
Autor:
Sidney Pitt, Sylwia Stachura, Rosemary Zhang, Steven G. Nadler, Kim W. McIntyre, Hong Wu, James Kempson, Jonathan Lippy, John Hynes, Joel C. Barrish, Zhonghui Lu, Percy H. Carter, Gary L. Schieven, Bin Jiang, Kate Gillooly, William J. Pitts, Javed Khan, Stephen T. Wrobleski, Jingwu Duan, Aberra Fura, Guoxiang Shen, John S. Tokarski, John S. Sack, Luisa Salter-Cid
Publikováno v:
Bioorganicmedicinal chemistry letters. 27(14)
A series of potent dual JAK1/3 inhibitors have been developed from a moderately selective JAK3 inhibitor. Substitution at the C6 position of the pyrrolopyridazine core with aryl groups provided exceptional biochemical potency against JAK1 and JAK3 wh
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::253daa677cbcba359ab77a6e70a14d27
https://pubmed.ncbi.nlm.nih.gov/28539220
https://pubmed.ncbi.nlm.nih.gov/28539220
Autor:
Kevin Kish, Tianle Li, Shuqun Lin, Yi Fan, Alaric J. Dyckman, John H. Dodd, Murray McKinnon, Rosemary Zhang, John S. Sack, Katerina Leftheris, John S. Tokarski, T. G. Murali Dhar, Gary L. Schieven, Susan E. Kiefer, Arthur M. Doweyko, Joel C. Barrish, Mark R. Witmer, Stephen T. Wrobleski, Sidney Pitt, John A. Newitt
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:4120-4126
A novel series of p38 MAP kinase inhibitors with high selectivity for the p38α isoform over the other family members including the highly homologous p38β isoform has been identified. X-ray co-crystallographic studies have revealed an unprecedented
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3f28c8e396ac76e6111c1f403141f812
https://doi.org/10.1016/j.bmcl.2013.05.047
https://doi.org/10.1016/j.bmcl.2013.05.047
Autor:
Rosemary Zhang, Mary F. Malley, Sidney Pitt, John S. Sack, Gary L. Schieven, Susan E. Kiefer, Stephen T. Wrobleski, John A. Newitt, James M. Trzaskos, Kevin Kish, Shuqun Lin, Joel C. Barrish, John H. Dodd, Murray McKinnon, Katerina Leftheris, John Hynes, Arthur M. Doweyko, Yi Fan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:5864-5868
The design, synthesis, and structure–activity relationships (SAR) of a series of 2-aminothiazol-5-yl-pyrimidines as novel p38α MAP kinase inhibitors are described. These efforts led to the identification of 41 as a potent p38α inhibitor that util
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0c09b23115c3b132f803f180d2db1d1d
https://doi.org/10.1016/j.bmcl.2010.07.102
https://doi.org/10.1016/j.bmcl.2010.07.102
Autor:
Shuqun Lin, David J. Shuster, John H. Dodd, Sidney Pitt, Murray McKinnon, Jeffrey Tredup, Stephen T. Wrobleski, Katerina Leftheris, John Hynes, Joel C. Barrish, Kim W. McIntyre, Arthur M. Doweyko, Kathleen M. Gillooly, Rosemary Zhang, John S. Sack, Gary L. Schieven, Hong Wu, Ding Ren Shen, Kevin Kish, Gerald J. Duke
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:2739-2744
A novel series of compounds based on the pyrrolo[2,1-f][1,2,4]triazine ring system have been identified as potent p38 alpha MAP kinase inhibitors. The synthesis, structure-activity relationships (SAR), and in vivo activity of selected analogs from th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b2533f563fa794b746e1d47aa4bac6a6
https://doi.org/10.1016/j.bmcl.2008.02.067
https://doi.org/10.1016/j.bmcl.2008.02.067
Autor:
David J. Shuster, Kevin Kish, Hongjian Zhang, Joel C. Barrish, Kathleen M. Gillooly, Sidney Pitt, Kim W. McIntyre, Xiao Xia Yang, John H. Dodd, Tracy L. Taylor, Murray McKinnon, John S. Sack, Katerina Leftheris, John Hynes, Rosemary Zhang, Punit Marathe, Gary L. Schieven, Susan E. Kiefer, Hong Wu, Ding Ren Shen, Arthur M. Doweyko, John A. Newitt
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:1762-1767
A novel structural class of p38alpha MAP kinase inhibitors has been identified via iterative SAR studies of a focused deck screen hit. Optimization of the lead series generated 6e, BMS-640994, a potent and selective p38alpha inhibitor that is orally
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::26f7e53e3f92698b2b6cc9d789e3375c
https://doi.org/10.1016/j.bmcl.2008.02.031
https://doi.org/10.1016/j.bmcl.2008.02.031
Autor:
Bang-Chi Chen, Suhong Pang, Steven H. Spergel, Leslie Leith, David J. Shuster, John Wityak, Derek J. Norris, Jagabandhu Das, Rulin Zhao, Gary L. Schieven, Kim W. McIntyre, Joel C. Barrish, Rosemary Zhang, Kamelia Behnia, Ding Ren Shen, Sidney Pitt, Arthur M. Doweyko, Ping Chen, Henry F. De Fex
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:6061-6066
A series of substituted 2-(aminoheteroaryl)-thiazole-5-carboxamide analogs have been synthesized as novel, potent inhibitors of the Src-family kinase p56Lck. Among them, compound 2 displayed superior in vitro potency and excellent in vivo efficacy.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7b919dd207e6828284c8e329093d65a0
https://doi.org/10.1016/j.bmcl.2004.09.093
https://doi.org/10.1016/j.bmcl.2004.09.093
Autor:
John Wityak, Amrita Kamath, Louis J. Lombardo, Ping Chen, John T. Hunt, Ivan Inigo, Stephen Castaneda, Joel C. Barrish, Herbert E. Klei, Robert J. Schmidt, John S. Tokarski, Sidney Pitt, Derek J. Norris, Francis Y. Lee, Jagabandhu Das, Craig Fairchild, Kathy A. Johnston, Punit Marathe, Robert M. Borzilleri, Cornelius Lyndon A M, Suhong Pang, Mei-Li Wen, Russell Peterson, Gary L. Schieven, Kamelia Behnia, David Kan, Arthur M. Doweyko
Publikováno v:
Journal of Medicinal Chemistry. 47:6658-6661
A series of substituted 2-(aminopyridyl)- and 2-(aminopyrimidinyl)thiazole-5-carboxamides was identified as potent Src/Abl kinase inhibitors with excellent antiproliferative activity against hematological and solid tumor cell lines. Compound 13 was o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::368da0e6e3d35ffae3cb0ff13f42526f
https://doi.org/10.1021/jm049486a
https://doi.org/10.1021/jm049486a