Zobrazeno 1 - 10
of 12
pro vyhledávání: '"Thomas P. Maduskuie"'
Autor:
Swamy Yeleswaram, Jason Boer, Sharon Diamond, Nikoo Falahatpisheh, Thomas P. Maduskuie, Yu Li
Publikováno v:
Drug Metabolism and Disposition. 38:1277-1285
An investigation was conducted to follow up on the apparent species-dependent toxicity reported for 6-(6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-ylthio)quinoline (SGX523), a mesenchymal-epithelial transition factor (c-MET) inhibi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5e8204b1a475cf97c1eb11c9a2319b50
https://doi.org/10.1124/dmd.110.032375
https://doi.org/10.1124/dmd.110.032375
Autor:
Kim L. R. Brouwer, Lauren E. Richards, Carl P. Decicco, Frank W. Lee, C. Edwin Garner, Hao Xiong, Gang Luo, Jingwu Duan, Thomas P. Maduskuie, Hanbo Hu, Liang Shang Gan, Helen Shen
Publikováno v:
Drug Metabolism and Disposition. 35:835-840
DPC 333 [(2R)-2-{(3R)-3-amino-3-[4-(2-methylquinolin-4-ylmethoxy)phenyl]-2-oxopyrrolidin-1-yl}-N-hydroxy-4-methylpentanamide] is a potent human tumor necrosis factor alpha-converting enzyme inhibitor with potential therapeutic implications for rheuma
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3804ca05378ff71848e1b496e37d989f
https://doi.org/10.1124/dmd.106.013946
https://doi.org/10.1124/dmd.106.013946
Autor:
Ruth R. Wexler, Hollis Smith Kezar, Edward S. Shimshick, Jeffrey T. Billheimer, C. Anne Higley, Richard G. Wilde, Peter J. Gillies, Sandra J. Germain, Thomas P. Maduskuie
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:167-172
A series of compounds bearing heterocyclic substituents were prepared, and evaluated for inhibition of the ACAT enzyme. The heterocyclic groups were compared in terms of in vitro potency against their diarylimidazole analogues. Data for the purposes
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::831190fc822fe70a18a6f283b9ab4ede
https://doi.org/10.1016/0960-894x(95)00001-a
https://doi.org/10.1016/0960-894x(95)00001-a
Autor:
Peter J. Gillies, C. Anne Higley, Pennio Pennev, Alexander L. Johnson, Candy S. Robinson, Richard G. Wilde, Thomas P. Maduskuie, Jeffrey T. Billheimer, Ruth R. Wexler
Publikováno v:
Journal of Medicinal Chemistry. 37:3511-3522
A series of 4,5-diaryl-2-(substituted thio)-1H-imidazoles has been synthesized and demonstrated to be potent inhibitors of acyl-CoA:cholesterol acyltransferase (ACAT). The design, synthesis, and structure-activity relationships for this series are re
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::384606c84f7d1f655086b272c98237d8
https://doi.org/10.1021/jm00047a009
https://doi.org/10.1021/jm00047a009
Autor:
Ruth R. Wexler, Jeffrey T. Billheimer, Peter J. Gillies, E. S. Shimshick, Sandra J. Germain, H. S. Iii Kezar, C. A. Higley, Richard G. Wilde, Thomas P. Maduskuie
Publikováno v:
ChemInform. 26
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::ca2a064fcf0bf49a0bc39f191abe7042
https://doi.org/10.1002/chin.199524260
https://doi.org/10.1002/chin.199524260
Autor:
Howard S. Shapiro, Victor Giulio Matassa, David Aharony, David W. Snyder, Barrie Hesp, Thomas P. Maduskuie, Richard A. Keith, Robert D. Krell
Publikováno v:
Journal of Medicinal Chemistry. 33:1781-1790
1,3,5-Substituted indoles and indazoles have been studied as receptor antagonists of the peptidoleukotrienes. The best of these compounds generally had a methyl group at the N1 position, a [(cyclopentyloxy)carbonyl]amino or 2-cyclopentylacetamido or
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9d0e96f35f04c091f3cfde2d7a481549
https://doi.org/10.1021/jm00168a037
https://doi.org/10.1021/jm00168a037
Autor:
Yuzhong Deng, Thomas P. Maduskuie, Jingwu Duan, Maryanne B. Covington, Bernice Brogdon, Mingxin Qian, Michael J Fossler, Kris Vaddi, C. Edwin Garner, James M. Trzaskos, Jing-Tao Wu, Richard Q. Liu, Stephen A. Bai, Robert Newton, David D. Christ, Carl P. Decicco
Publikováno v:
Drug metabolism and disposition: the biological fate of chemicals. 35(10)
DPC 333 ((2R)-2-((3R)-3-amino-3{4-[2-methyl-4-quinolinyl) methoxy] phenyl}-2-oxopyrrolidinyl)-N-hydroxy-4-methylpentanamide)) is a potent and selective inhibitor of tumor necrosis factor (TNF)-alpha-converting enzyme (TACE). It significantly inhibits
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d7718fa747a54076f5168e1d736de737
https://pubmed.ncbi.nlm.nih.gov/17656469
https://pubmed.ncbi.nlm.nih.gov/17656469
Autor:
Qian Wang, Kris Vaddi, Wenqing Yao, Song Mei, Chu-Biao Xue, Kamna Katiyar, Yun-Long Li, Maryanne B. Covington, Peggy Scherle, Brent Douty, Niu Shin, Holly Koblish, Sybil O'Connor, Sharon Diamond-Fosbenner, Yu Li, Andrew P. Combs, Eddy W. Yue, Reid Huber, Xin He, Leslie Hall, Kathy Wang, Patricia Feldman, Robert C. Newton, Yanlong Li, Swamy Yeleswaram, Thomas P. Maduskuie
Publikováno v:
Cancer Research. 75:2671-2671
Phosphatidylinositol 3-kinases (PI3Ks) belong to a family of lipid signaling kinases that phosphorylate phosphatidylinositol-4,5-bisphosphate (PIP2), giving rise to phosphatidylinositol-3,4,5-triphosphate (PIP3). PIP3 functions as a second messenger
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e3dd673d41b144ffb2bb7cb34f66f2e9
https://doi.org/10.1158/1538-7445.am2015-2671
https://doi.org/10.1158/1538-7445.am2015-2671
Autor:
Mercy Ramanjulu, Ann Y. Liauw, Thomas P. Maduskuie, Jere E. Meredith, Jeffrey N. Higaki, Robert Zaczek, Barbara Cordell, Arthur H. Roach, Dietmar A. Seiffert, David Robertson, Padmaja Kasireddy-Polam, Lorin A. Thompson, Marcie A. Glicksman, Stephen E. Mercer, Andrew P. Combs, Richard E. Olson, Rui-Qin Liu
Publikováno v:
Bioorganicmedicinal chemistry letters. 16(9)
The synthesis, evaluation, and structure-activity relationships of a series of succinoyl lactam inhibitors of the Alzheimer's disease gamma-secretase are described. Beginning with a screening hit with broad proteinase activity, optimization provided
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::15589f134d4cb016d3cf88127c79f08f
https://pubmed.ncbi.nlm.nih.gov/16473009
https://pubmed.ncbi.nlm.nih.gov/16473009
Autor:
Pancras C. Wong, Pieter F. W. Stouten, Matthew R. Wright, Karen A. Rossi, Richard S. Alexander, Robert A. Galemmo, Robert M. Knabb, Thomas P. Maduskuie, Bruce J. Aungst, Ruth R. Wexler, Brian L. Wells, Celia Dominguez
Publikováno v:
Bioorganicmedicinal chemistry letters. 10(3)
In this report refinements to the S4 ligand group leads to compound 19, an inhibitor of fXa with good potency in vitro and an improved pharmacokinetic profile in rabbit. The X-ray crystallographic study of a representative analogue confirms our bindi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6ea135050341b9d6cb3dddaaf9c6c02b
https://pubmed.ncbi.nlm.nih.gov/10698459
https://pubmed.ncbi.nlm.nih.gov/10698459