Hsingan Tsai
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Explore the profile of Hsingan Tsai including associated specialties, affiliations and a list of published articles.
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7
Citations
39
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Recent Articles
1.
Chelliah M, Eagen K, Guo Z, Chackalamannil S, Xia Y, Tsai H, et al.
ACS Med Chem Lett
. 2014 Jun;
5(5):561-5.
PMID: 24900880
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....
2.
Xia Y, Chackalamannil S, Clasby M, Doller D, Eagen K, Greenlee W, et al.
Bioorg Med Chem Lett
. 2007 Jun;
17(16):4509-13.
PMID: 17574850
The structure-activity relationship (SAR) of the vinyl pyridine region of himbacine derived thrombin receptor (PAR-1) antagonists is described. A 2-vinylpyridyl ring substituted with an aryl or a heteroaryl group at...
3.
Clasby M, Chackalamannil S, Czarniecki M, Doller D, Eagen K, Greenlee W, et al.
Bioorg Med Chem Lett
. 2007 May;
17(13):3647-51.
PMID: 17490877
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...
4.
Clasby M, Chackalamannil S, Czarniecki M, Doller D, Eagen K, Greenlee W, et al.
J Med Chem
. 2007 Jan;
50(1):129-38.
PMID: 17201416
The metabolism of our prototypical thrombin receptor antagonist 1, Ki = 2.7 nM, was studied and three major metabolites (2, 4, and 5) were found. The structures of the metabolites...
5.
Xia Y, Chackalamannil S, Chan T, Czarniecki M, Doller D, Eagen K, et al.
Bioorg Med Chem Lett
. 2006 Jul;
16(18):4969-72.
PMID: 16824760
The structure-activity relationship (SAR) of the lactone ring of himbacine derived thrombin receptor (PAR-1) antagonists (e.g., 2-5) is described. The effect of the lactone carbonyl group on binding to PAR-1...
6.
Clasby M, Chackalamannil S, Czarniecki M, Doller D, Eagen K, Greenlee W, et al.
Bioorg Med Chem Lett
. 2005 Dec;
16(6):1544-8.
PMID: 16380251
The design, synthesis, and SAR studies of a structurally novel series of highly potent thrombin receptor (PAR-1) antagonists are described. Compound 30 is a highly potent thrombin receptor antagonist (IC(50)=6.3...
7.
Chackalamannil S, Xia Y, Greenlee W, Clasby M, Doller D, Tsai H, et al.
J Med Chem
. 2005 Sep;
48(19):5884-7.
PMID: 16161991
Structurally novel thrombin receptor (protease activated receptor 1, PAR-1) antagonists based on the natural product himbacine are described. The prototypical PAR-1 antagonist 55 showed a Ki of 2.7 nM in...