Zobrazeno 1 - 10 of 23 pro vyhledávání: '"Joseph J. Nunes"'
2
Discovery of oxazolo[4,5-b]pyridines and related heterocyclic analogs as novel SIRT1 activators
Autor: David P. Carney, Amy V. Lynch, Robert B. Perni, Pui Yee Ng, Jeremy S. Disch, Roger Xie, Michael R. Jirousek, Jill C. Milne, J. Joshua Smith, Lei Jin, Andre Iffland, Joseph J. Nunes, Jean Bemis, Siva Lavu, Chi B. Vu
Publikováno v: Bioorganic & Medicinal Chemistry Letters. 19:2350-2353
SIRT1 is an NAD+-dependent protein deacetylase that appears to produce beneficial effects on metabolic parameters such as glucose and insulin homeostasis. Activation of SIRT1 by resveratrol (1) has been shown to modulate insulin resistance, increase
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6f244e63f7cbed43f6d57bb08bab4ff2
https://doi.org/10.1016/j.bmcl.2008.11.106
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3
Discovery of Imidazo[1,2-b]thiazole Derivatives as Novel SIRT1 Activators
Autor: Philip D. Lambert, David J. Gagne, Joseph J. Nunes, Jerrold M. Olefsky, Jean Bemis, Chi B. Vu, Jill C. Milne, Amy V. Lynch, J. Joshua Smith, David P. Carney, Michael R. Jirousek, Robert B. Perni, Pui Yee Ng, Jeremy S. Disch, Simon Schenk, Siva Lavu
Publikováno v: Journal of Medicinal Chemistry. 52:1275-1283
A series of imidazo[1,2-b]thiazole derivatives is shown to activate the NAD(+)-dependent deacetylase SIRT1, a potential new therapeutic target to treat various metabolic disorders. This series of compounds was derived from a high throughput screening
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1f7c6857bfb9e2c4e77d9cfa1518e2e0
https://doi.org/10.1021/jm8012954
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6
Discovery of novel 2,3-diarylfuro[2,3-b]pyridin-4-amines as potent and selective inhibitors of Lck: Synthesis, SAR, and pharmacokinetic properties
Autor: Ryan White, David C. Mcgowan, Xiaotian Zhu, Matthew W. Martin, John Newcomb, John L. Buchanan, Theodore Faust, Faye Hsieh, Xin Huang, Erin F. DiMauro, Susan M. Turci, Christina Boucher, Stephen Schneider, Joseph J. Nunes, Jean Bemis, Josie H. Lee
Publikováno v: Bioorganic & Medicinal Chemistry Letters. 17:2299-2304
2,3-Diarylfuro[2,3-b]pyridine-4-amines are a novel class of potent and selective inhibitors of Lck. The discovery, synthesis, and structure activity relationships of this series of inhibitors are reported. The most promising compounds were also profi
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4cec8aa93efe43539a086c398621a2de
https://doi.org/10.1016/j.bmcl.2007.01.048
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9
N-(3-(phenylcarbamoyl)arylpyrimidine)-5-carboxamides as potent and selective inhibitors of Lck: structure, synthesis and SAR
Autor: Alan C. Cheng, Stephen Schneider, Joseph J. Nunes, Xiaotian Zhu, Paul Gallant, Erin F. DiMauro, Xin Huang, Vinod F. Patel, John Newcomb, Brian L. Hodous, Holly L. Deak, Christina Boucher, Susan M. Turci, Josie H. Lee, Linda F. Epstein
Publikováno v: Bioorganicmedicinal chemistry letters. 18(3)
N-3-(Phenylcarbamoyl)arylpyrimidine-5-carboxamides are a novel class of selective Lck inhibitors. This series of compounds derives its selectivity from a hydrogen bond with the gatekeeper Thr316 of the enzyme. X-ray co-crystal structural data, struct
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a79e72e4e6984650f09152ff1fcc2fe7
https://pubmed.ncbi.nlm.nih.gov/18083554
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10
Discovery of 4-amino-5,6-biaryl-furo[2,3-d]pyrimidines as inhibitors of Lck: development of an expedient and divergent synthetic route and preliminary SAR
Autor: Alan C. Cheng, Ryan White, Stephen Schneider, Joseph J. Nunes, John L. Buchanan, Jean Bemis, Faye Hsieh, William H. Buckner, Susan M. Turci, Matthew W. Martin, Christina Boucher, John Newcomb, Xin Huang, Xiaotian Zhu, Josie H. Lee, Theodore Faust, Erin F. DiMauro, David C. Mcgowan, Teresa L. Marshall
Publikováno v: Bioorganicmedicinal chemistry letters. 17(8)
4-Amino-5,6-biaryl-furo[2,3-d]pyrimidines were identified as potent non-selective inhibitors of Lck. A novel, divergent, and practical synthetic route was developed to access derivatives from bifunctional intermediates. Lead optimization was guided b
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d8596032c12f0ec265ab314e83b4a1d9
https://pubmed.ncbi.nlm.nih.gov/17280833
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