Zobrazeno 1 - 6
of 6
pro vyhledávání: '"Jeffrey Deignan"'
Autor:
Lawrence R. McGee, Jeffrey T. Mihalic, Yingcai Wang, Mei-Chu Lo, Jing Zhou, Steven H. Olson, Xiaoqi Chen, Frank Kayser, Jiang Zhu, Ada Chen, Jeffrey Deignan, Jonathan D. Oliner, Alexander M. Long, Daqing Sun, Ming Yu, Xin Huang, Qiuping Ye, Jiwen Jim Liu, Peter Yakowec, Julio C. Medina
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:3782-3785
We recently reported on the discovery of AMG 232, a potent and selective piperidinone inhibitor of the MDM2-p53 interaction. AMG 232 is being evaluated in human clinical trials for cancer. Continued exploration of the N-alkyl substituent of this seri
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cb62da92063f4e1d74dae97a63a686bb
https://doi.org/10.1016/j.bmcl.2014.06.073
https://doi.org/10.1016/j.bmcl.2014.06.073
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:
Mei-Chu Lo, Ji Ma, Julio C. Medina, Dineli Wickramasinghe, Mark L. Ragains, Derek E. Piper, Merrill Ayres, Zhihong Li, Alex J. Zhang, Xiaoqi Chen, Jeffrey Deignan, Zhulun Wang, Kanaka Pattabiraman, Kathleen S. Keegan, Xiaoning Zhao, Rachel Ngo, Nigel Walker, Lingming Liang, Margaret F. Weidner, Paul M. Wehn, Christophe Queva, Jason Duquette, Alexander Kamb, Ada Chen, Malgorzata Wanska, Jeffrey T. Mihalic, Kriti Modi, Pingchen Fan, Grace Q. Alba, Yunxiao Li, Michael W. Gribble, John Eksterowicz, Jacob Kaizerman, Dustin McMinn, Xianghong Wang, Michael DeGraffenreid, Steve Thibault, Xiaodong Wang, Kexue Li, Benjamin Fisher, Richard V. Connors, Wen Liu, Sarah E. Lively, Cong Li, Kang Dai, Jiasheng Fu, Justin N. Huard, Robert Cho, Lawrence R. McGee, Timothy J. Carlson, Julia Suchomel
Publikováno v:
Journal of medicinal chemistry. 57(8)
We describe the structural optimization of a lead compound 1 that exhibits dual inhibitory activities against FLT3 and CDK4. A series of pyrido[4',3':4,5]pyrrolo[2,3-d]pyrimidine derivatives was synthesized, and SAR analysis, using cell-based assays,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5055c042d7a9cff8f5682847cec87995
https://pubmed.ncbi.nlm.nih.gov/24641103
https://pubmed.ncbi.nlm.nih.gov/24641103
Autor:
Felix Gonzalez-Lopez de Turiso, Ada Chen, Steven H. Olson, Xin Huang, Jude Canon, Anne Y. Saiki, Michael D. Bartberger, Hilary Plake Beck, Jonathan D. Oliner, David J. Kopecky, Xuelei Yan, Jing Zhou, Maria M. Toteva, Min Jiang, Mei-Chu Lo, Alexander M. Long, Darin J. Gustin, Klaus Michelsen, Tao Osgood, Steve Schneider, Qiuping Ye, Jeffrey Deignan, Yosup Rew, Peter Yakowec, Daqing Sun, Xianyun Jiao, Lixia Jin, Dongyin Yu, David Chow, Julio C. Medina, Frank Kayser, Mark L. Ragains, Yihong Li, Xiaoning Zhao, Brian M. Fox
Publikováno v:
Journal of medicinal chemistry. 55(11)
Structure-based rational design led to the discovery of novel inhibitors of the MDM2–p53 protein–protein interaction. The affinity of these compounds for MDM2 was improved through conformational control of both the piperidinone ring and the appen
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4e801db16462f352d2d21a52ca43e600
https://pubmed.ncbi.nlm.nih.gov/22624960
https://pubmed.ncbi.nlm.nih.gov/22624960
Autor:
Valerie D Stowell, Dale L. Barnard, Donald F. Smee, M Kim Nielsen, Hongwei Yuan, Lihui Sun, Hua Cao, Jeffrey Deignan, Clay Quint, Jennifer Crabb, Ailing Li, Michael T. Flavin, Robert W. Sidwell, Ze-Qi Xu, Raghu Samy
Publikováno v:
Animal, Dairy, and Veterinary Science Faculty Publications
A series of coumarin and pyranocoumarin analogues were evaluated in vitro for antiviral efficacy against measles virus (MV), strain Chicago. Of the 22 compounds tested for inhibition, six were found to have selectivity indices greater than 10. These
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5ace9398ba4929bd119df6abe2df7a45
https://pubmed.ncbi.nlm.nih.gov/12180648
https://pubmed.ncbi.nlm.nih.gov/12180648