Zobrazeno 1 - 10
of 17
pro vyhledávání: '"Hsingan Tsai"'
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
Autor:
Keith Eagen, Dario Doller, Martin C. Clasby, Andrew T. McPhail, Hsingan Tsai, Yan Xia, Yan Lin, Samuel Chackalamannil
Publikováno v:
Tetrahedron Letters. 41:4043-4047
An efficient, multigram-scale synthesis of dihydronaphthofuranone 1 using a novel aryl intramolecular Diels–Alder reaction of propargyl trans -cinnamate 8 is described. Catalytic reduction of 1 gave the cis -fused tetrahydronaphthofuranone derivati
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::23479ab5d4cf6cfb7aa4e5c0385b3217
https://doi.org/10.1016/s0040-4039(00)00585-2
https://doi.org/10.1016/s0040-4039(00)00585-2
Autor:
Vaccaro Henry A, Ahmad Fawzi, Hongtao Zhang, Robert W. Watkins, Hsingan Tsai, Renee Cleven, Yan Xia, Michael Czarniecki, John Cook, Samuel Chackalamannil
Publikováno v:
Journal of Medicinal Chemistry. 40:4372-4377
Polycyclic pyrazolo[3,4-d]pyrimidines (represented by 3 and 4) were synthesized as analogues of the recently reported polycyclic guanine phosphodiesterase (PDE) inhibitors. From the structure-activity relationship (SAR) development of a series of com
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e7ab3cfbcb9b39372752b5d8ff5d5313
https://doi.org/10.1021/jm970495b
https://doi.org/10.1021/jm970495b
Autor:
Ho-Sam Ahn, Ana Bercovici, George Boykow, Alan Bronnenkant, Samuel Chackalamannil, Jason Chow, Renee Cleven, John Cook, Michael Czarniecki, Carol Domalski, Ahmad Fawzi, Michael Green, Asli Gündes, Ginny Ho, Malvina Laudicina, Neil Lindo, Ke Ma, Mahua Manna, Brian McKittrick, Bita Mirzai, Terry Nechuta, Bernard Neustadt, Chester Puchalski, Kathryn Pula, Lisa Silverman, Elizabeth Smith, Andrew Stamford, Richard P. Tedesco, Hsingan Tsai, Deen Tulshian, Henry Vaccaro, Robert W. Watkins, Xiaoyu Weng, Joseph T. Witkowski, Yan Xia, Hongtao Zhang
Publikováno v:
Journal of Medicinal Chemistry. 40:2196-2210
Tetracyclic guanines have been shown to be potent and selective inhibitors of the cGMP-hydrolyzing enzymes PDE1 and PDE5. In general, these compounds are inactive or only weakly active as inhibitors of PDE3, which is a major isozyme involved in cAMP
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a0abf0b24745580e391dbef2bfd691d2
https://doi.org/10.1021/jm9608467
https://doi.org/10.1021/jm9608467
Autor:
Andrew Stamford, Ahmad Fawzi, Yuguang Wang, Michael Czarniecki, Hsingan Tsai, Samuel Chackalamannil, Shin Chung, Mckittrick Brian A, Renee Cleven
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 6:1257-1260
Phosphinic acid derivatives, represented by structure 1 , have been synthesized and evaluated as endothelin converting enzyme (ECE) inhibitors. Several of these compounds (for example, 1b , 1c , and 1f ) were found to be potent inhibitors of ECE with
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::35554cb9ed2005078af364d400887e38
https://doi.org/10.1016/0960-894x(96)00211-9
https://doi.org/10.1016/0960-894x(96)00211-9
Autor:
Suke Wang, Hsingan Tsai, Samuel Chackalamannil, Yuguang Wang, Yan Xia, George Boykow, Michael Czarniecki, Ho-Sam Ahn, Anthony Clemmons
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:2005-2010
The synthesis and CETP inhibitory activity of a series of compounds related to wiedendiols ( 1a,1b ) are reported. It is proposed that a two point pharmacophore consisting of a catechol group and a large hydrophobic anchor is necessary for activity.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::69af780ffcf334f40791f7a1cc7c3ffe
https://doi.org/10.1016/0960-894x(95)00342-q
https://doi.org/10.1016/0960-894x(95)00342-q
Autor:
Samuel Chackalamannil, Ahmad Fawzi, Mckittrick Brian A, Yuguang Wang, Michael Czarniecki, Hsingan Tsai, Shin Chung, Andrew Stamford, Renee Cleven
Publikováno v:
ChemInform. 27
Phosphinic acid derivatives, represented by structure 1 , have been synthesized and evaluated as endothelin converting enzyme (ECE) inhibitors. Several of these compounds (for example, 1b , 1c , and 1f ) were found to be potent inhibitors of ECE with
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e716998cd6332739a451eab5d4b9bf98
https://doi.org/10.1002/chin.199642211
https://doi.org/10.1002/chin.199642211
Autor:
Vaccaro Henry A, Robert W. Watkins, Yan Xia, Hsingan Tsai, Renee Cleven, Hongtao Zhang, Ahmad Fawzi, Michael Czarniecki, Samuel Chackalamannil, John Cook
Publikováno v:
ChemInform. 29
Polycyclic pyrazolo[3,4-d]pyrimidines (represented by 3 and 4) were synthesized as analogues of the recently reported polycyclic guanine phosphodiesterase (PDE) inhibitors. From the structure−activ...
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::d07fd0c0ce96dedd4f8997670e569639
https://doi.org/10.1002/chin.199820191
https://doi.org/10.1002/chin.199820191
Autor:
Andrew T. McPhail, Keith Eagen, Yan Xia, Yan Lin, Hsingan Tsai, Martin C. Clasby, Samuel Chackalamannil, Dario Doller
Publikováno v:
ChemInform. 31
An efficient, multigram-scale synthesis of dihydronaphthofuranone 1 using a novel aryl intramolecular Diels–Alder reaction of propargyl trans -cinnamate 8 is described. Catalytic reduction of 1 gave the cis -fused tetrahydronaphthofuranone derivati
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::d035998dea99ab207e4d7e1a36ddba54
https://doi.org/10.1002/chin.200035095
https://doi.org/10.1002/chin.200035095