Zobrazeno 1 - 10
of 26
pro vyhledávání: '"John J. Piwinski"'
Autor:
Xu Han, Yang Mei, Rama K. Mishra, Honghao Bi, Atul D. Jain, Gary E. Schiltz, Baobing Zhao, Madina Sukhanova, Pan Wang, Arabela A. Grigorescu, Patricia C. Weber, John J. Piwinski, Miguel A. Prado, Joao A. Paulo, Len Stephens, Karen E. Anderson, Charles S. Abrams, Jing Yang, Peng Ji
Publikováno v:
The Journal of Clinical Investigation, Vol 133, Iss 6 (2023)
Myeloproliferative neoplasms (MPNs) are characterized by the activated JAK2/STAT pathway. Pleckstrin-2 (Plek2) is a downstream target of the JAK2/STAT5 pathway and is overexpressed in patients with MPNs. We previously revealed that Plek2 plays critic
Externí odkaz:
https://doaj.org/article/2701d1efe9e540b6893f0cff3edaf376
Autor:
Jeremy Clark, Xiao Tong, Ashok Arasappan, Randall R. Rossman, Anita T. Fowler, Subramaniam Ananthan, Vinay Girijavallabhan, Feng Geng, Regina Huelgas, Neng-Yang Shih, F. George Njoroge, Hollis S. Kezar, Joseph A. Maddry, Yuhua Huang, Frank Bennett, Cheng Li, John J. Piwinski, Cecil D. Kwong, John A. Secrist, Stephanie Curry, Abhijit Roychowdhury, Malcolm MacCoss, Robert C. Reynolds, Hsueh-Cheng Huang, Robert Chase
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:5144-5149
Introduction of nitrogen atom into the benzene ring of a previously identified HCV replication (replicase) benzofuran inhibitor 2, resulted in the discovery of the more potent pyridofuran analogue 5. Subsequent introduction of small alkyl and alkoxy
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a19a20c57978b9eb8444e2b3affa03ce
https://doi.org/10.1016/j.bmcl.2012.06.021
https://doi.org/10.1016/j.bmcl.2012.06.021
Autor:
Ashok Arasappan, Seong-Heon Kim, Robert C. Reynolds, Cheng Li, Aneta Kosinski, Jeremy Clark, Joseph A. Kozlowski, Ling Tong, Vinay Girijavallabhan, Pinto Patrick A, Lei Chen, F. George Njoroge, Anita T. Fowler, Vishal Verma, Subramaniam Ananthan, Randall R. Rossman, Robert Chase, Neng-Yang Shih, Joseph A. Maddry, John A. Secrist, Cecil D. Kwong, Hollis S. Kezar, Abhijit Roychowdhury, Stephanie Curry, Malcolm MacCoss, Hsueh-Cheng Huang, Razia Rizvi, Frank Bennett, Stephen Gavalas, Yuhua Huang, Francisco Velazquez, Alvarez Carmen S, Feng Geng, Xiao Tong, John J. Piwinski, Regina Huelgas, Bandarpalle B. Shankar, Srikanth Venkatraman
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:3229-3234
Based on a previously identified HCV replication (replicase) inhibitor 1 , SAR efforts were conducted around the pyrimidine core to improve the potency and pharmacokinetic profile of the inhibitors. A benzothiazole moiety was found to be the optimal
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::63e593455015b9cae754dc9b1385747b
https://doi.org/10.1016/j.bmcl.2012.03.036
https://doi.org/10.1016/j.bmcl.2012.03.036
Autor:
Neng-Yang Shih, Joseph A. Maddry, Xiao Tong, Subramaniam Ananthan, Cheng Li, Jeremy Clark, Feng Geng, Hollis S. Kezar, Cecil D. Kwong, John J. Piwinski, Abhijit Roychowdhury, Robert C. Reynolds, Anita T. Fowler, Ashok Arasappan, Hsueh-Cheng Huang, John A. Secrist, F. George Njoroge, Boris Feld
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:1160-1164
Compound 1 was identified as a HCV replication inhibitor from screening/early SAR triage. Potency improvement was achieved via modulation of substituent on the 5-azo linkage. Due to potential toxicological concern, the 5-azo linkage was replaced with
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5a01a2091efa205ec0a5d00edbf54a02
https://doi.org/10.1016/j.bmcl.2011.11.091
https://doi.org/10.1016/j.bmcl.2011.11.091
Autor:
Peter Orth, Bandarpalle B. Shankar, Daniel Lundell, Corey O. Strickland, Vinay Girijavallabhan, Chaoyang Dai, Joseph A. Kozlowski, Janeta Popovici-Muller, Brian J. Lavey, Jing Sun, Shiying Chen, Dansu Li, John J. Piwinski, Razia Rizvi, M. Arshad Siddiqui, Kristin E. Rosner, Lianyun Zhao, Zhuyan Guo, Wong Michael K C, Neng-Yang Shih, Xiaoda Niu
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:3172-3176
TNF-α converting enzyme (TACE) inhibitors are promising agents to treat inflammatory disorders and cancer. We have investigated novel tartrate diamide TACE inhibitors where the tartrate core binds to zinc in a unique tridentate fashion. Incorporatin
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b5ffe3fdf02a5dba0580b311b55f7fe2
https://doi.org/10.1016/j.bmcl.2011.01.002
https://doi.org/10.1016/j.bmcl.2011.01.002
Autor:
Liping Yang, Shelby Umland, Peter Orth, Daniel Lundell, Luke Firmansjah, Feltz Robert, Chaoyang Dai, Joseph A. Kozlowski, Wensheng Yu, Janeta Popovici-Muller, Seong Heon Kim, Vincent S. Madison, John J. Piwinski, De-Yi Yang, M. Arshad Siddiqui, Ling Tong, Xiaoda Niu, Brian J. Lavey, Guowei Zhou, Banderpalle B. Shankar, Razia Rizvi, Kristin E. Rosner, Neng-Yang Shih, Aneta Kosinski, Hong Bian, Dansu Li, Vinay Girijavallabhan, Lei Chen, Himanshu Shah, Zhuyan Guo, Jing Sun, Wong Michael K C
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:7283-7287
Our research on hydantoin based TNF-α converting enzyme (TACE) inhibitors has led to an acetylene containing series that demonstrates sub-nanomolar potency (K(i)) as well as excellent activity in human whole blood. These studies led to the discovery
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1f13e3eb17b7abab77da7bd68ad794d7
https://doi.org/10.1016/j.bmcl.2010.10.081
https://doi.org/10.1016/j.bmcl.2010.10.081
Autor:
Bandarpalle B. Shankar, Ling Tong, Himanshu Shah, Wensheng Yu, Jing Sun, De-Yi Yang, Guowei Zhou, Lei Chen, Feltz Robert, Kristin E. Rosner, Xiaoda Niu, Neng-Yang Shih, Shelby Umland, Zhuyan Guo, John J. Piwinski, Seong Heon Kim, Dansu Li, Razia Rizvi, Peter Orth, Aneta Kosinski, Wong Michael K C, Joseph A. Kozlowski, Daniel Lundell, M. Arshad Siddiqui, Brian J. Lavey
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:5286-5289
We disclose further optimization of hydantoin TNF-alpha convertase enzyme (TACE) inhibitors. SAR with respect to the non-prime region of TACE active site was explored. A series of biaryl substituted hydantoin compounds was shown to have sub-nanomolar
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0544f42865077bfcb9c1747073ba2311
https://doi.org/10.1016/j.bmcl.2010.06.134
https://doi.org/10.1016/j.bmcl.2010.06.134
Autor:
Jing Sun, Corey O. Strickland, John P. Caldwell, Kristin E. Rosner, Pauline C. Ting, Bandarpalle B. Shankar, Shiying Chen, David B. Belanger, Gerald W. Shipps, Vinay Girijavallabhan, Guowei Zhou, Brian J. Lavey, Dansu Li, Razia Rizvi, Peter Orth, Neng-Yang Shih, M. Arshad Siddiqui, Zhaoning Zhu, Wensheng Yu, Zhuyan Guo, Zhidan Liu, Maria David, John J. Piwinski, Daniel Lundell, Henry M. Vaccaro, Joe F. Lee, Jim Spitler, Vincent S. Madison, Xiaoda Niu, Chaoyang Dai, Mckittrick Brian A, Joseph A. Kozlowski, Janeta Popovici-Muller, Rob Mazzola
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:4812-4815
The syntheses and structure-activity relationships of the tartrate-based TACE inhibitors are discussed. The optimization of both the prime and non-prime sites led to compounds with picomolar activity. Several analogs demonstrated good rat pharmacokin
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::78b8670bf1029b4ff13b82406eff8483
https://doi.org/10.1016/j.bmcl.2010.06.104
https://doi.org/10.1016/j.bmcl.2010.06.104
Autor:
Jacob Valiyaveettil, Vinay Girijavallabhan, Pinto Patrick A, Lei Chen, Seong-Heon Kim, Anita T. Fowler, Cecil D. Kwong, Neng-Yang Shih, Xiao Tong, Cheng Li, Frank Bennett, Namita Bansal, Joseph A. Maddry, Hsueh-Cheng Huang, Subramaniam Ananthan, Ling Tong, Stephanie Curry, Joseph A. Kozlowski, Malcolm MacCoss, Srikanth Venkatraman, Francisco Velazquez, Hollis S. Kezar, Bandarpalle B. Shankar, Alvarez Carmen S, Vishal Verma, Randall R. Rossman, John J. Piwinski, Yuhua Huang, Robert C. Reynolds, Stephen Gavalas, Razia Rizvi, Robert Chase, Aneta Kosinski, Ashok Arasappan, John A. Secrist, Jeremy Clark, F. George Njoroge
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(17)
Introduction of a nitrogen atom into the benzene ring of a previously identified HCV replication (replicase) benzothiazole inhibitor 1 , resulted in the discovery of the more potent pyridothiazole analogues 3 . The potency and PK properties of the co
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::12b8f85f4ca4fda22394ea622aca8cb0
https://pubmed.ncbi.nlm.nih.gov/22858143
https://pubmed.ncbi.nlm.nih.gov/22858143
Autor:
Pauline C. Ting, Motasim Billah, Ji Zhang, Peng Wang, Daniel Prelusky, David J. Blythin, John H. Schwerdt, John J. Piwinski, Ling Lin, Li Xiao, Xiao Chen, Xiang Zhang, Ho-Jane Shue, Neng-Yang Shih, Jianhua Cao, Ping Wu, Chander S. Celly, Rongze Kuang, Robert G. Aslanian, Danlin Gu
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(7)
Optimization of oxazole-based PDE4 inhibitors has led to the discovery of a series of quinolyl oxazoles, with 4-benzylcarboxamide and 5-α-aminoethyl groups which exhibit picomolar potency against PDE4. Selectivity profiles and in vivo biological act
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::76ef660ee57e97c99ba25220cea0146f
https://pubmed.ncbi.nlm.nih.gov/22401864
https://pubmed.ncbi.nlm.nih.gov/22401864