Zobrazeno 1 - 10
of 69
pro vyhledávání: '"Ho-Sam Ahn"'
Autor:
Keith Eagen, Yunsheng Hsieh, Mariappan V. Chelliah, Stan Kurowski, Zhuyan Guo, Madhu Chintala, William J. Greenlee, Hsingan Tsai, Samuel Chackalamannil, Ho-Sam Ahn, Yan Xia, George Boykow
Publikováno v:
ACS Medicinal Chemistry Letters. 5:561-565
We have synthesized several C7-spirocyclic analogues of vorapaxar and evaluated their in vitro activities against PAR-1 receptor. Some of these analogues showed activities and rat plasma levels comparable to vorapaxar. Compound 5c from this series sh
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5167ac4b35159c9670df81e0eaf948e6
https://doi.org/10.1021/ml500008w
https://doi.org/10.1021/ml500008w
Autor:
Stan Kurowski, Mariappan V. Chelliah, William J. Greenlee, Madhu Chintala, Yunsheng Hsieh, Yan Xia, George Boykow, Ho-Sam Ahn, Samuel Chackalamannil
Publikováno v:
ACS Medicinal Chemistry Letters. 5:183-187
We have synthesized several C7-aminomethyl analogues of vorapaxar that are potent PAR-1 antagonists. Many of these analogues showed excellent in vitro binding affinity and pharmacokinetics profile in rats. Compound 6a from this series showed excellen
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::64b51fb9c036df9fa0fa9ec39ff0de40
https://doi.org/10.1021/ml400452v
https://doi.org/10.1021/ml400452v
Autor:
Mariappan V. Chelliah, Tze-Ming Chan, Yan Xia, George Boykow, Madhu Chintala, Matthew Bryant, Ho-Sam Ahn, Keith Eagen, Jacqueline Agans-Fantuzzi, William J. Greenlee, Yunsheng Hsieh, Samuel Chackalamannil
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:2544-2549
Discovery of a novel nor-seco himbacine analog as potent thrombin receptor (PAR-1) antagonist is described. Despite low plasma level, these new analogs showed excellent ex vivo efficacy in the monkey platelet aggregation assay. A potent hydroxy metab
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e94036f493fa5d675af5fc8cc2d8746b
https://doi.org/10.1016/j.bmcl.2012.01.138
https://doi.org/10.1016/j.bmcl.2012.01.138
Autor:
Ho-Sam Ahn, Jacqueline Agans-Fantuzzi, Matthew Bryant, Chan Tze-Ming, George Boykow, Yan Xia, Keith Eagen, David Hesk, Madhu Chintala, Mariappan V. Chelliah, Yunsheng Hsieh, Martin C. Clasby, Xiaobang Gao, Jairam Palamanda, William J. Greenlee, Samuel Chackalamannil
Publikováno v:
Journal of Medicinal Chemistry. 50:5147-5160
Pursuing our earlier efforts in the himbacine-based thrombin receptor antagonist area, we have synthesized a series of compounds that incorporate heteroatoms in the C-ring of the tricyclic motif. This effort has resulted in the identification of seve
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::59cc61ee2f05b48391d822d3acecca21
https://doi.org/10.1021/jm070704k
https://doi.org/10.1021/jm070704k
Autor:
Keith Eagen, Andrew T. McPhail, William J. Greenlee, Yunsheng Hsieh, Madhu Chintala, Samuel Chackalamannil, Yan Lin, Hsingan Tsai, Jayaram R. Tagat, Dario Doller, Ho-Sam Ahn, Yan Xia, George Boykow, Martin C. Clasby, Jacqueline Agans-Fantuzzi, Michael Czarniecki
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:3647-3651
The synthesis and biological activity of a novel series of thrombin receptor antagonists is described. This series of compounds showed excellent in vitro and in vivo potency. The most potent compound 40 had an IC(50) of 7.6 nM and showed robust inhib
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::314b4325d14e742098e88c8f15d4faa6
https://doi.org/10.1016/j.bmcl.2007.04.061
https://doi.org/10.1016/j.bmcl.2007.04.061
Autor:
George Boykow, Samuel Chackalamannil, Andrew T. McPhail, Hsingan Tsai, William J. Greenlee, Yan Xia, Dario Doller, Ho-Sam Ahn, Michael Czarniecki, Yuguang Wang, Tze-Ming Chan, Keith Eagen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:4969-4972
The structure–activity relationship (SAR) of the lactone ring of himbacine derived thrombin receptor (PAR-1) antagoinsts (e.g., 2 – 5 ) is described. The effect of the lactone carbonyl group on binding to PAR-1 is dependent on the substitution pa
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5fe9b4e7cde9221168fb8b70ce95de0e
https://doi.org/10.1016/j.bmcl.2006.06.042
https://doi.org/10.1016/j.bmcl.2006.06.042
Publikováno v:
Current Pharmaceutical Design. 9:2349-2365
Thrombin, a plasma serine protease, plays a key role not only in coagulation and hemostasis but in thrombosis, restenosis and atherosclerosis. Thrombin activates platelets, endothelium, inflammatory cells and smooth muscle cells. The cellular action
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::78e68a0eb7315a73934ab84d2250475f
https://doi.org/10.2174/1381612033453884
https://doi.org/10.2174/1381612033453884
Publikováno v:
Current Medicinal Chemistry-Cardiovascular & Hematological Agents. 1:37-45
Protease activated receptor-1 (PAR-1), also known as thrombin receptor, is present in a variety of cell types such as platelets and endothelial cells. PAR-1 is proteolytically activated by thrombin by cleavage at its extracellular domain, unmasking a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ae4dff68371f83cadcd3e7b62f988243
https://doi.org/10.2174/1568016033356706
https://doi.org/10.2174/1568016033356706
Publikováno v:
Biochemical Pharmacology. 60:1425-1434
A growing body of evidence suggests an important contribution of the cellular actions of thrombin to thrombosis and restenosis following angioplasty. Recently we reported on SCH 79797 ( N 3-cyclopropyl-7-{[4-(1-methylethyl)phenyl]methyl}-7 H -pyrrolo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::416f9117b7a155cd4957da1e97a0c166
https://doi.org/10.1016/s0006-2952(00)00460-3
https://doi.org/10.1016/s0006-2952(00)00460-3
Autor:
Mary Ann Caplen, Andrew Stamford, Carolyn Foster, Yusheng Wu, Ho-Sam Ahn, George Boykow, Duane A. Burnett, Leyla Arik, Martin S. Domalski, Mahua Manna, Michael Czarniecki
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 9:2073-2078
A series of pyrroloquinazolines has been discovered that represent novel small molecule inhibitors of the intramolecular ligand of the thrombin receptor. Analogs were prepared to study the structure-activity relationships of substitution at the N 1,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f136f86334731fdae2e53defb686ddda
https://doi.org/10.1016/s0960-894x(99)00339-x
https://doi.org/10.1016/s0960-894x(99)00339-x