Zobrazeno 1 - 10
of 16
pro vyhledávání: '"Jason Duquette"'
Autor:
Iain D. G. Campuzano, Xiaolin Hao, Brian Lucas, Tisha San Miguel, Deanna Mohn, Kirk Henne, Benjamin Fisher, Minna Bui, Mario G. Cardozo, Robert S. Foti, Ron C. Kelly, Christine Vissinga, Thuy B. Tran, John D. McCarter, Leeanne Zalameda, Daniela Metz, Douglas A. Whittington, Sharon Wannberg, Yi-Ling Hu, John Whoriskey, Julio C. Medina, Felix Gonzalez-Lopez de Turiso, Timothy D. Cushing, Xuxia Zhang, Lawrence R. McGee, Michael G. Johnson, Xiao He, Gang Yu, Michelle C. Dunn, Jason Duquette, Youngsook Shin
Publikováno v:
Journal of Medicinal Chemistry. 59:7252-7267
Optimization of the potency and pharmacokinetic profile of 2,3,4-trisubstituted quinoline, 4, led to the discovery of two potent, selective, and orally bioavailable PI3Kδ inhibitors, 6a (AM-0687) and 7 (AM-1430). On the basis of their improved profi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::5b68313a948b3dc2d85bb6149f781869
https://doi.org/10.1021/acs.jmedchem.6b00827
https://doi.org/10.1021/acs.jmedchem.6b00827
Autor:
Jason Duquette, Xin Huang, Dongyin Yu, Yun Ling, Jing Zhou, Yu Chung Wang, Daqing Sun, Sarah Wortman, John Eksterowicz, Qiuping Ye, Min Jiang, Jonathan D. Oliner, Lixia Jin, Alexander M. Long, Ana Z. Gonzalez, Peter Yakowec, Yihong Li, Steven H. Olson, Anne Y. Saiki, Hilary Plake Beck, Yosup Rew, Lawrence R. McGee, Julio C. Medina, Jonathan B. Houze, Jiasheng Fu, Jude Canon, Mcintosh Joel, Ada Chen, Brian M. Fox, Mei-Chu Lo, Xuelei Yan, Paul L. Shaffer, Zhihong Li, Tao Osgood, Xiaoning Zhao
Publikováno v:
Journal of Medicinal Chemistry. 57:10499-10511
Structure-based rational design and extensive structure-activity relationship studies led to the discovery of AMG 232 (1), a potent piperidinone inhibitor of the MDM2-p53 association, which is currently being evaluated in human clinical trials for th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a6411aa1211e82e797ec19f5aeedd623
https://doi.org/10.1021/jm501550p
https://doi.org/10.1021/jm501550p
Autor:
Andrew Tasker, Andreas Reichelt, Yi-Ling Hu, Deanna Mohn, John McCarter, Ben Fisher, Robert M. Rzasa, Yi Chen, Julio C. Medina, Gang Yu, Sharon Wannberg, Brian Lucas, Ron C. Kelly, Jennifer Seganish, Felix Gonzalez-Lopez de Turiso, Xiaolin Hao, Kristin L. Andrews, Douglas A. Whittington, Matthew Frank Brown, Dawei Zhang, Youngsook Shin, Mario G. Cardozo, Jason Duquette, Robert C. Wahl, Leeanne Zalameda, Daniela Metz, Vatee Pattaropong, Michael G. Johnson, Tisha San Miguel, Randall W. Hungate, John Whoriskey, Lawrence R. McGee, Timothy D. Cushing, Kirk Henne, Liping H. Pettus, Xiao He
Publikováno v:
Journal of Medicinal Chemistry. 58:480-511
The development and optimization of a series of quinolinylpurines as potent and selective PI3Kδ kinase inhibitors with excellent physicochemical properties are described. This medicinal chemistry effort led to the identification of 1 (AMG319), a com
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::41f464b8458b3d559ce036ed30580e01
https://doi.org/10.1021/jm501624r
https://doi.org/10.1021/jm501624r
Autor:
Ada Chen, Steven H. Olson, Alexander M. Long, John Eksterowicz, Michael D. Bartberger, Jing Zhou, Yosup Rew, Lawrence R. McGee, Mei-Chu Lo, Anne Y. Saiki, Dongyin Yu, Jason Duquette, Xuelei Yan, Ana Z. Gonzalez, Hilary Plake Beck, Jonathan B. Houze, Yun Ling, Mcintosh Joel, Jonathan D. Oliner, Sarah Wortman, Jude Canon, Daqing Sun, Dustin McMinn, Brian M. Fox, Paul L. Shaffer, Xiaoning Zhao, Tao Osgood, Lixia Jin, Xin Huang, Zhihong Li, David Chow, Qiuping Ye, Yihong Li, Jiasheng Fu, Peter Yakowec, Julio C. Medina
Publikováno v:
Journal of Medicinal Chemistry. 57:2472-2488
We previously reported the discovery of AMG 232, a highly potent and selective piperidinone inhibitor of the MDM2-p53 interaction. Our continued search for potent and diverse analogues led to the discovery of novel morpholinone MDM2 inhibitors. This
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::de1d3d1db724c5401afea1de13f776b9
https://doi.org/10.1021/jm401767k
https://doi.org/10.1021/jm401767k
Autor:
Felix, Gonzalez-Lopez de Turiso, Xiaolin, Hao, Youngsook, Shin, Minna, Bui, Iain D G, Campuzano, Mario, Cardozo, Michelle C, Dunn, Jason, Duquette, Benjamin, Fisher, Robert S, Foti, Kirk, Henne, Xiao, He, Yi-Ling, Hu, Ron C, Kelly, Michael G, Johnson, Brian S, Lucas, John, McCarter, Lawrence R, McGee, Julio C, Medina, Daniela, Metz, Tisha, San Miguel, Deanna, Mohn, Thuy, Tran, Christine, Vissinga, Sharon, Wannberg, Douglas A, Whittington, John, Whoriskey, Gang, Yu, Leeanne, Zalameda, Xuxia, Zhang, Timothy D, Cushing
Publikováno v:
Journal of medicinal chemistry. 59(15)
Optimization of the potency and pharmacokinetic profile of 2,3,4-trisubstituted quinoline, 4, led to the discovery of two potent, selective, and orally bioavailable PI3Kδ inhibitors, 6a (AM-0687) and 7 (AM-1430). On the basis of their improved profi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::a242cbf7d7efba8c63b94dcec247686e
https://pubmed.ncbi.nlm.nih.gov/27411843
https://pubmed.ncbi.nlm.nih.gov/27411843
Autor:
Jason Duquette, Johann Chan, Darin J. Gustin, An-Rong Li, Xiaoqi Chen, Jeff Deignan, Julio C. Medina, Xiaohui Du, George Tonn, Tim Sullivan, Jeffrey T. Mihalic, Bryan Lemon, Kirk Henne, Shichang Miao, Michael Johnson, Zice Fu, Ji Ma, Tassie L. Collins
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:357-362
The optimization of a series of 8-aza-quinazolinone analogs for antagonist activity against the CXCR3 receptor is reported. Compounds were optimized to avoid the formation of active metabolites and time-dependent-inhibitors of CYP3A4. In addition, an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::339aed731e6cb3461777050b365762b1
https://doi.org/10.1016/j.bmcl.2011.10.120
https://doi.org/10.1016/j.bmcl.2011.10.120
Autor:
Jason Duquette, Emmanuel Sabalan, Ji Ma, Xiaoqi Chen, Shichang Miao, Julio C. Medina, Darin J. Gustin, Zhulun Wang, Lawrence R. McGee, Kirk Henne, Tassie L. Collins, George Tonn, Karen Ebsworth, Tim Sullivan, Xiaohui Du, Bryan Lemon
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:5200-5204
A general way of improving the potency of CXCR3 antagonists with fused hetero-bicyclic cores was identified. Optimization efforts led to the discovery of a series of imidazo-pyrazine derivatives with improved pharmacokinetic properties in addition to
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::32b84253576b3d5672e7b511fae6245c
https://doi.org/10.1016/j.bmcl.2009.07.021
https://doi.org/10.1016/j.bmcl.2009.07.021
Autor:
Jason Duquette, Lawrence R. McGee, Xiaohui Du, Tim Sullivan, Julio C. Medina, Jay Danao, George Tonn, Michael G. Johnson, Darin J. Gustin, Zice Fu, Jeffrey Deignan, Ji Ma, Liusheng Zhu, Liang Tang, Andrew P. Marcus, An-Rong Li, Phillipe Bergeron, Xiaoqi Chen, Bryan Lemon, Jiwen Liu, Tassie L. Collins, Teresa Arazas Carabeo, Jeffrey T. Mihalic
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:688-693
A series of six–six and six–five fused heterocyclic CXCR3 antagonists has been synthesized and their activities evaluated in an [125I]-IP-10 displacement assay and an ITAC mediated in vitro cell migration assay. The pharmacokinetic properties of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::56a2bd5999bfd49a8e8a6ca4e4ac43a4
https://doi.org/10.1016/j.bmcl.2007.11.060
https://doi.org/10.1016/j.bmcl.2007.11.060
Autor:
Jason Duquette, Xiaoqi Chen, George Tonn, Jeffrey T. Mihalic, Julio C. Medina, Ji Ma, Shichang Miao, Karen Ebsworth, Jeffrey Deignan, An-Rong Li, Tassie L. Collins, Xiaohui Du, Bryan Lemon, Tim Sullivan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:608-613
A series of imidazole derivatives have been designed and optimized for CXCR3 antagonism, pharmacokinetic properties, and reduced formation of glutathione conjugates. Our efforts led to the discovery of potent CXCR3 antagonists with good pharmacokinet
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f5a9a60c5206e6e66c7bd4d6a6702a47
https://doi.org/10.1016/j.bmcl.2007.11.072
https://doi.org/10.1016/j.bmcl.2007.11.072
Autor:
Yi-Ling Hu, Leeanne Zalameda, Daniela Metz, Julia Suchomel, Thuy B. Tran, Gang Yu, Jason Duquette, John McCarter, Xuxia Zhang, Youngsook Shin, Simon Wong, Julio C. Medina, Sharon Wannberg, Timothy D. Cushing, Tisha San Miguel, Mario G. Cardozo, Lawrence R. McGee, Ron C. Kelly, Christine Vissinga, Deanna Mohn, John Whoriskey, Douglas A. Whittington, Kirk Henne, Xiao He
Publikováno v:
Journal of medicinal chemistry. 59(1)
Lead optimization efforts resulted in the discovery of two potent, selective, and orally bioavailable PI3Kδ inhibitors, 1 (AM-8508) and 2 (AM-9635), with good pharmacokinetic properties. The compounds inhibit B cell receptor (BCR)-mediated AKT phosp
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3bd418762bb2f427cfe73c0b9127b325
https://pubmed.ncbi.nlm.nih.gov/26652588
https://pubmed.ncbi.nlm.nih.gov/26652588