Zobrazeno 1 - 10
of 34
pro vyhledávání: '"Roland Burli"'
Autor:
Zaher ElBeck, Mohammad Bakhtiar Hossain, Humam Siga, Nikolay Oskolkov, Fredrik Karlsson, Julia Lindgren, Anna Walentinsson, Dominique Koppenhöfer, Rebecca Jarvis, Roland Bürli, Tanguy Jamier, Elske Franssen, Mike Firth, Andrea Degasperi, Claus Bendtsen, Robert I. Menzies, Katrin Streckfuss-Bömeke, Michael Kohlhaas, Alexander G. Nickel, Lars H. Lund, Christoph Maack, Ákos Végvári, Christer Betsholtz
Publikováno v:
Nature Communications, Vol 15, Iss 1, Pp 1-23 (2024)
Abstract While excessive production of reactive oxygen species (ROS) is a characteristic hallmark of numerous diseases, clinical approaches that ameliorate oxidative stress have been unsuccessful. Here, utilizing multi-omics, we demonstrate that in c
Externí odkaz:
https://doaj.org/article/8cb734f3e6db454ca663dbe7df2cc0bb
Autor:
Jeffrey H. Kogan, Samer Chmait, Chun Li, Essa Hu, Michelle Lindstrom, Jiandong Zhang, Kristin L. Andrews, Roland Burli, Roxanne Kunz, Stephen Hitchcock, James J. S. Treanor, Ning Chen, Shannon Rumfelt
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:2262-2265
We report the discovery of 6,7-dimethoxy-4-(pyridin-3-yl)cinnolines as novel inhibitors of phosphodiesterase 10A (PDE10A). Systematic examination and analyses of structure–activity-relationships resulted in single digit nM potency against PDE10A. X
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::865cbcb6f0a332d88ba4d4befabc0a9d
https://doi.org/10.1016/j.bmcl.2012.01.086
https://doi.org/10.1016/j.bmcl.2012.01.086
Autor:
Min Wong, Yang Xu, Scot Middleton, Matthew R. Lee, Anu Gore, Mike Fiorino, Alex Pickrell, Kristine M. Muller, Andrea Itano, Mike Frohn, Heather A. Arnett, Janet Buys, Michelle Horner, Dalia Rivenzon-Segal, Jennifer E. Golden, Victor J. Cee, Hugo M. Vargas, Roland Burli, Susana C. Neira, Michael Schrag, Han Xu, Brian A. Lanman, Michele McElvain, Xuxia Zhang, Jerry Siu
Publikováno v:
ACS Medicinal Chemistry Letters. 2:107-112
The optimization of a series of thiazolopyridine S1P1 agonists with limited activity at the S1P3 receptor is reported. These efforts resulted in the discovery of 1-(3-fluoro-4-(5-(1-phenylcyclopropyl)thiazolo-[5,4-b]pyridin-2-yl)benzyl)azetidine-3-ca
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::469aac7dbf0531b12b4eec83f252b55d
https://doi.org/10.1021/ml100306h
https://doi.org/10.1021/ml100306h
Autor:
Hugo M. Vargas, Yang Xu, Jerry Siu, Janet Buys, Michelle Horner, Jian Lin, Ashis Saha, Han Xu, Michele McElvain, Anurag Sharadendu, Scot Middleton, Roland Burli, Yael Marantz, Dalia Segal, Kevin Salyers, Mercedes Lobera, Dilara Mccauley, Srinivas Chereku, Xiang Yu, Nili Schutz, Michael Schrag
Publikováno v:
ACS Medicinal Chemistry Letters. 2:97-101
We have discovered novel benzofuran-based S1P1 agonists with excellent in vitro potency and selectivity. 1-((4-(5-Benzylbenzofuran-2-yl)-3-fluorophenyl)methyl) azetidine-3-carboxylic acid (18) is a potent S1P1 agonist with >1000× selectivity over S1
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ff8291efcc95ecdaf3a6ce8e57343599
https://doi.org/10.1021/ml100227q
https://doi.org/10.1021/ml100227q
Autor:
Jennifer E. Golden, Randall W. Hungate, Alexander J. Pickrell, Gloria Biddlecome, Roland Burli, Mike Frohn, Jennifer Dao, Norma Rogers, Vellarkad N. Viswanadhan, Jennifer R. Allen, Kristine M. Muller, Sean Yoder
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:5023-5026
We report the structure-based design and synthesis of a novel series of aza-benzimidazoles as PHD2 inhibitors. These efforts resulted in compound 22, which displayed highly potent inhibition of PHD2 function in vitro.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f6fe8ee6a4b24c934b0f90897c408cc8
https://doi.org/10.1016/j.bmcl.2008.08.012
https://doi.org/10.1016/j.bmcl.2008.08.012
Autor:
Randall W. Hungate, Jennifer Dao, Christopher M. Tegley, Sean Yoder, Catherine H. Chang, Tanya Peterkin, Roland Burli, Henrike Veith, Jennifer R. Allen, Philip Tagari, Norma Rogers, Kaustav Biswas, Vellarkad N. Viswanadhan, Michael J. Frohn, Gloria Biddlecome
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:3925-3928
Inhibition of the PHD2 enzyme has been associated with increased red blood cell levels. From a screening hit, a series of novel hydroxyl-thiazoles were developed as potent PHD2 inhibitors.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1b45d47469e72a7c165facd5f7029bbb
https://doi.org/10.1016/j.bmcl.2008.06.031
https://doi.org/10.1016/j.bmcl.2008.06.031
Autor:
Ning Chen, Andrea Itano, Randall W. Hungate, Ryan White, Yang Xu, Matthew H. Plant, Yanyan Tudor, Yen Nguyen, Roxanne Kunz, Perry M. Novak, Kristin Meagher, Essa Hu, Jason Brooks Human, Shaun Flynn, Gordon Ng, Xuxia Zhang, Violeta Yu, Roland Burli, Douglas A. Whittington, Andrew Tasker
Publikováno v:
Journal of Medicinal Chemistry. 51:3065-3068
Inhibition of c-Kit has the potential to treat mast cell associated fibrotic diseases. We report the discovery of several aminoquinazoline pyridones that are potent inhibitors of c-Kit with greater than 200-fold selectivity against KDR, p38, Lck, and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::81447f11bfae7a4d16eb01799010756e
https://doi.org/10.1021/jm800188g
https://doi.org/10.1021/jm800188g
Publikováno v:
Synlett. 2008:1005-1008
Selective 2-hydroxyethylation at the N-1 position of benzyl 5-methyl-3-oxo-2-phenyl-2,3-dihydro-1 H-pyrazole-4-carboxylate with epoxides was achieved using either AlMe 3 or Mg(ClO 4 ) 2 under mild conditions. The epoxide ring opening was both regiose
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::dad9fe261ec74d9a661a6714c0e1cb8f
https://doi.org/10.1055/s-2008-1042923
https://doi.org/10.1055/s-2008-1042923
Publikováno v:
Tetrahedron Letters. 49:794-798
The regioselective, copper-catalyzed coupling of a tautomeric pyrazolone/pyrazole with 2-halopyridines was investigated. Conditions were developed to preferentially form either the N-aryl or O-aryl product.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::20de58f596f180be7b399be54df34465
https://doi.org/10.1016/j.tetlet.2007.11.185
https://doi.org/10.1016/j.tetlet.2007.11.185
Autor:
Kelly Regal, Randall W. Hungate, Mike Frohn, Vellarkad N. Viswanadhan, Matthew Adlam, Han Xu, Philip Tagari, Min Wong, Kristine M. Muller, Roland Burli, Jennifer E. Golden, Xiaoming Zou, Matthew H. Plant, Michele McElvain
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:3713-3718
We report the discovery of potent agonists for the human formyl-peptide-like 1 receptor (hFPRL1). These compounds did not act at a closely related receptor denoted human formyl peptide receptor (hFPR) up to 10 microM concentration. Recent studies hav
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d19e4048cb68caaf96dd2c0a6c5b8b6a
https://doi.org/10.1016/j.bmcl.2006.04.068
https://doi.org/10.1016/j.bmcl.2006.04.068