Zobrazeno 1 - 10 of 16 pro vyhledávání: '"Stanley Kugler"'
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Structural studies unravel the active conformation of apo RORγt nuclear receptor and a common inverse agonism of two diverse classes of RORγt inhibitors
Autor: Xiang Li, Robert Hughes, Charles Kennedy, Brian Nicholas Cook, Stanley Kugler, Ingo Muegge, Delphine Collin, John Wan, Marie Anderson, Mark E. Labadia, Donna Terenzio, Neil A. Farrow, Siqi Lin, Debra L. Brennan
Publikováno v: Journal of Biological Chemistry. 292:11618-11630
The nuclear receptor retinoid acid receptor-related orphan receptor γt (RORγt) is a master regulator of the Th17/IL-17 pathway that plays crucial roles in the pathogenesis of autoimmunity. RORγt has recently emerged as a highly promising target fo
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cd028be21b18235969de935bcc1a90d4
https://doi.org/10.1074/jbc.m117.789024
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4
Indole RSK inhibitors. Part 2: Optimization of cell potency and kinase selectivity
Autor: Mohammed A. Kashem, Stanley Kugler, Lida Soleymanzadeh, Yunlong Zhang, Jeffery B. Madwed, Xin Guo, Kirrane Thomas M, Roger J. Snow, Alan David Swinamer, Jennifer Burke, Margaret M. O’Neill, Stephen J. Boyer
Publikováno v: Bioorganic & Medicinal Chemistry Letters. 22:738-742
A series of inhibitors for the 90 kDa ribosomal S6 kinase (RSK) based on an 1-oxo-2,3,4,5-tetrahydro-1H-[1,4]diazepino[1,2-a]indole-8-carboxamide scaffold were optimized for cellular potency and kinase selectivity. This led to the identification of c
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0e3a6710f1742d2d831246aeb83ce910
https://doi.org/10.1016/j.bmcl.2011.10.029
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5
Indole RSK inhibitors. Part 1: Discovery and initial SAR
Autor: Zhaoming Xiong, Stephen J. Boyer, Lida Soleymanzadeh, Stanley Kugler, John Westbrook, Yunlong Zhang, Anil Kumar Padyana, Jennifer Burke, Jeffrey B. Madwed, Derek Cogan, Alan David Swinamer, Chris Sarko, Mohammed A. Kashem, Frank M. DiCapua, Kirrane Thomas M, Amy Gao, Roger J. Snow, Xin Guo, Margaret M. O’Neill
Publikováno v: Bioorganic & Medicinal Chemistry Letters. 22:733-737
A series of inhibitors for the 90 kDa ribosomal S6 kinase (RSK) based on an 1-oxo-2,3,4,5-tetrahydro-1H-[1,4]diazepino[1,2-a]indole-8-carboxamide scaffold were identified through high throughput screening. An RSK crystal structure and exploratory SAR
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::280d6ba59ece0c6b1b215b764b652158
https://doi.org/10.1016/j.bmcl.2011.10.030
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6
Substituted 2H-isoquinolin-1-ones as potent Rho-kinase inhibitors: Part 2, optimization for blood pressure reduction in spontaneously hypertensive rats
Autor: Stanley Kugler, John D. Ginn, Xiang Li, Todd Bosanac, Mohammed A. Kashem, Steven Kerr, Anthony S. Prokopowicz, Michael Robert Turner, Frank Wu, Erick R. R. Young, James D. Smith, Eugene R. Hickey, Sabine Schlyer, Charles L. Cywin, Rhonda Chen
Publikováno v: Bioorganic & Medicinal Chemistry Letters. 20:5153-5156
Phenylglycine substituted isoquinolones 1 and 2 have previously been described as potent dual ROCK1/ROCK2 inhibitors. Here we describe the further SAR of this series to improve metabolic stability and rat oral exposure. Piperidine analog 20 which dem
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2c1691612ce33705cab799aaae34b250
https://doi.org/10.1016/j.bmcl.2010.07.014
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7
Substituted 2H-isoquinolin-1-one as potent Rho-Kinase inhibitors. Part 1: Hit-to-lead account
Autor: Steven Kerr, Charles L. Cywin, Frank H. Büttner, Frank Wu, Mohammed A. Kashem, Scott Jakes, Zofia Paw, Roger J. Snow, Erick R. R. Young, Eugene R. Hickey, Stanley Kugler, Paul Kaplita, Cheng-Kon Shih, Rhonda Chen, Anthony S. Prokopowicz
Publikováno v: Bioorganic & Medicinal Chemistry Letters. 20:3235-3239
Two closely related scaffolds were identified through an uHTS campaign as desirable starting points for the development of Rho-Kinase (ROCK) inhibitors. Here, we describe our hit-to-lead evaluation process which culminated in the rapid discovery of p
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3c2d691a0169d6458e981f329be40c8b
https://doi.org/10.1016/j.bmcl.2010.04.070
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8
Discovery of 1,3-dihydro-2,1,3-benzothiadiazole 2,2-dioxide analogs as new RORC modulators
Autor: Stanley Kugler, Yunlong Zhang, Melissa Hill-Drzewi, Ingo Muegge, Lana Smith, Delphine Collin, Josh Horan, Xiang Li, Mark E. Labadia, Brian Nicholas Cook
Publikováno v: Bioorganicmedicinal chemistry letters. 25(9)
Structure-based and pharmacophore-based virtual screening in combination with combinatorial chemistry and X-ray crystallography led to the discovery of a new class of benzothiadiazole dioxide analogs with functional activity as RORC inverse agonists.
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::76908aa9df44092150a8cca25c4a5a4a
https://pubmed.ncbi.nlm.nih.gov/25840886
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10
Substituted 2H-isoquinolin-1-ones as potent Rho-kinase inhibitors: part 3, aryl substituted pyrrolidines
Autor: Steven Kerr, Erick R. R. Young, Eugene R. Hickey, Todd Bosanac, Alan Olague, John D. Ginn, Sabine Schlyer, Stanley Kugler, Xiang Li, Mohammed A. Kashem
Publikováno v: Bioorganicmedicinal chemistry letters. 20(12)
The discovery and SAR of a series of beta-aryl substituted pyrrolidine 2H-isoquinolin-1-one inhibitors of Rho-kinase (ROCK) derived from 2 is herein described. SAR studies have shown that aryl groups in the beta-position are optimal for potency. Our
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2f9c2c4f36334933f05f7838dd863ba1
https://pubmed.ncbi.nlm.nih.gov/20471253
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