Zobrazeno 1 - 10
of 34
pro vyhledávání: '"David E. Zembower"'
Autor:
Yasheen Zhou, Yongping Xie, Aye Aye Mar, Michael T. Flavin, Ali Koohang, David E. Zembower, Matthew M. Ames, Ze Qi Xu, Mary J. Kuffel, Rama K. Mishra
Publikováno v:
Anti-Cancer Agents in Medicinal Chemistry. 12:1117-1131
The indolo[2,3-a]carbazole alkaloids constitute an important class of natural products with interesting and diverse biological activities. A series of novel ring-fused indolocarbazoles were synthesized and evaluated for inhibition of topoisomerase I-
Autor:
Margret Thorsteinnsdottir, Alex S. Kiselyov, Gudmundur Sigthorsson, Rama K. Mishra, Jose Ramirez, Peng Yu, Nian Zhou, Jun Zhang, Emmanuel Onua, Mark E. Gurney, Georgeta Hategan, Thorkell Andresson, David E. Zembower, Wayne Zeller, Jasbir Singh, Alex Polozov
Publikováno v:
Journal of Medicinal Chemistry. 53:18-36
The EP3 receptor on the platelet mediates prostaglandin E2 potentiation of thrombogenic coagonists including collagen and adenosine diphosphate (ADP). A pharmacophore driven approach led to the identification of diverse peri-substituted heterocycles
Autor:
Gudrun Halldorsdottir, Gudmundur Sigthorsson, Heida Sigthorsdottir, Thorkell Andresson, Jennifer Winger, Emmanuel Onua, Livia A. Enache, Margret Thorsteinnsdottir, Bjorn Mamat, Douglas R. Davies, Jun Zhang, Monica Keyvan, David Sullins, Alex S. Kiselyov, Rama K. Mishra, Audur Thorlaksdottir, Li-Ming Zhou, David E. Zembower, Michael Krohn, Vincent Sandanayaka, Lance Stewart, Mark E. Gurney, Jasbir Singh
Publikováno v:
Journal of Medicinal Chemistry. 53:573-585
Both in-house human genetic and literature data have converged on the identification of leukotriene 4 hydrolase (LTA(4)H) as a key target for the treatment of cardiovascular disease. We combined fragment-based crystallography screening with an iterat
Autor:
Sergey Dzekhtser, Michael Krohn, Isaac Kennedy, Changren Yan, David E. Zembower, Glenn L. Stahl, Chen Wei, Robert A. Erickson, Livia A. Enache, Dragan Ristic, Alex S. Kiselyov, Frank W. Muellner, Vincent Sandanayaka, Jennifer Winger, David Sullins, Jasbir Singh
Publikováno v:
Organic Process Research & Development. 13:1177-1184
DG-051B is a first-in-class small molecule inhibitor of leukotriene A4 hydrolase (LTA4H), currently in Phase II clinical development for the prevention of heart attack. Process optimization led from a linear seven-step synthetic procedure to a conver
Autor:
Alex B. Burgin, Magnus H. Haraldsson, Brian Pease, Hidong Kim, Douglas R. Davies, Lance Stewart, David E. Zembower, Rama K. Mishra, Alex S. Kiselyov, Jasbir Singh, Jeff Christensen, Mark E. Gurney, Olafur T. Magnusson, Bjorn Mamat, Erik C Hansen
Publikováno v:
Journal of Medicinal Chemistry
We describe a novel fragment library termed fragments of life (FOL) for structure-based drug discovery. The FOL library includes natural small molecules of life, derivatives thereof, and biaryl protein architecture mimetics. The choice of fragments f
Peptide boronic acids Versatile synthetic ligands for affinity chromatography of serine proteinases*
Publikováno v:
International Journal of Peptide and Protein Research. 47:405-413
Peptide boronic acids are potent transition-state analogue inhibitors of serine proteinases. We prepared the peptide boronic acids Ala-Ala-boroPhe (AAbF), targeted at chymotrypsin-like proteinases, and Ala-Ala-boroVal (AAbV), targeted at elastolytic
Autor:
Matthew O'Connell, Livia A. Enache, Siead I. Zegar, David E. Zembower, Christopher J. Tokar, Wayne Zeller, Venkat Rajagopol, Frank W. Muellner, Jasbir Singh
Publikováno v:
Organic Process Research & Development. 11:747-753
DG-041 is a small molecule antagonist of the EP3 receptor for prostaglandin E2 that is in clinical development for treatment of peripheral artery disease (PAD). Originally produced using a six-step synthetic procedure, process optimization led to dev
Autor:
Nancy Jimenez, David E. Zembower, Michael T. Flavin, Eric W. Kirchhoff, Prabir Sen, and Ze-Qi Xu, Jintao Zhang
Publikováno v:
Organic Process Research & Development. 4:577-580
An automated process research approach to reaction optimization was developed. Chemical process research can be greatly accelerated by coupling automated synthesis equipment with statistical design of experiments (DoE). With the use of an automated p
Autor:
David E. Zembower, Heping Zhang
Publikováno v:
The Journal of Organic Chemistry. 63:9300-9305
Robustaflavone, a naturally occurring compound, is an inhibitor of hepatitis B virus replication in vitro. Robustaflavone is a biflavanoid composed of two units of apigenin (5,7,4‘-trihydroxyflavone) joined via a biaryl linkage between the 6-positi
Autor:
John D. Rizzo, Tracy L. Stup, Michael T. Flavin, Albert Khilevich, Robert W. Buckheit, Lin Lin, David E. Zembower, Ze-Qi Xu
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 8:2179-2184
The three chromanone derivatives, (+)-, (-)-, and (+/-)-12-oxocalanolide A (2), were evaluated for in vitro antiviral activities against HIV and simian immunodeficiency virus (SIV). The compounds were determined to be inhibitors of HIV-1 reverse tran