Zobrazeno 1 - 10
of 48
pro vyhledávání: '"John N, Freskos"'
Autor:
Amol Karwa, Bethel Asmelash, Kimberly R. Gaston, Carolyn J. Sympson, John N. Freskos, Bich Vu, Tim A. Marzan, Tasha M. Schoenstein, Thomas Rogers, Maureen A. Nickols
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:5566-5570
We describe the synthesis, MMP-2 and 9 potency, and in vitro evaluation of a series of α-sulfone hydroxmate MMP inhibitors conjugated to a series of dyes with different absorption/emission lamina maxima's that can be used to visualize tumors.
Autor:
Amolkumar Karwa, Carolyn J. Sympson, Michael A. Brown, John N. Freskos, Vladislav S. Golubkov, Carol Pearcy Howard, Arati D. Naik, Sergey A. Shiryaev, Alex Y. Strongin, Albert G. Remacle
Publikováno v:
Journal of Biological Chemistry. 288:20568-20580
Proteolytic activity of cell surface-associated MT1-matrix metalloproteinase (MMP) (MMP-14) is directly related to cell migration, invasion, and metastasis. MT1-MMP is regulated as a proteinase by activation and conversion of the latent proenzyme int
Autor:
Richard B. Dorshow, Bethel Asmelash, William L. Neumann, Jeng-Jong Shieh, Kimberly R. Gaston, John N. Freskos, Richard M. Fitch, Amruta R. Poreddy, Raghavan Rajagopalan, Karen P. Galen
Publikováno v:
Bioorganic & Medicinal Chemistry. 20:2490-2497
Novel pyrazine carboxamides bearing hydrophilic poly(ethylene glycol) (PEG) moieties were designed, synthesized, and evaluated for use as fluorescent glomerular filtration rate (GFR) tracer agents. Among these, compounds 4d and 5c that contain about
Autor:
Kimberly R. Gaston, Amruta R. Poreddy, Jeng-Jong Shieh, William L. Neumann, Richard M. Fitch, Bethel Asmelash, Karen P. Galen, Raghavan Rajagopalan, Richard B. Dorshow, John N. Freskos
Publikováno v:
Journal of Medicinal Chemistry. 54:5048-5058
Various hydrophilic pyrazine-bis(carboxamides) derived from 3,5-diamino-pyrazine-2,5-dicarboxylic acid bearing neutral and anionic groups were prepared and evaluated for use as fluorescent glomerular filtration rate (GFR) tracer agents. Among these,
Autor:
Sandra W. Curtiss, D. Joseph Rogier, Alan MacInnes, Brown David L, Mike B. Tollefson, Brian R. Bond, Yvette M. Fobian, Maddux Todd Michael, Dafydd R. Owen, Jeanne M. Rumsey, Brent V. Mischke, Jerry W. Cubbage, Alan G. Benson, Robert Hughes, Lena L Zhang, E. Jon Jacobsen, Steven E. Heasley, Joseph B. Moon, Ying Yu, John M. Molyneaux, Yi Zheng, Brad A. Acker, Blevis-Bal Radhika M, John N. Freskos, John K. Walker, Jennie L. Walgren
Publikováno v:
Journal of Medicinal Chemistry. 53:2656-2660
We recently described a novel series of aminopyridopyrazinones as PDE5 inhibitors. Efforts toward optimization of this series culminated in the identification of 3-[4-(2-hydroxyethyl)piperazin-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[
Autor:
Maddux Todd Michael, Yvette M. Fobian, Alan G. Benson, Dafydd R. Owen, Brian R. Bond, Christopher Phillips, Brad A. Acker, E. Jon Jacobsen, Michael John Palmer, D. Joseph Rogier, John M. Molyneaux, Brent V. Mischke, John N. Freskos, Tracy J. Ringer, Andrew Simon Bell, Blevis-Bal Radhika M, Robert Hughes, David G. Brown, Steve E. Heasley, Joseph B. Moon, John K. Walker, Brown David L, William C. Stallings, Michael B. Tollefson, Alan MacInnes, Jerry W. Cubbage, Yung Yu, Margarita Rodriquez-Lens, Fox David Nathan Abraham
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:4088-4091
A new class of potent and selective PDE5 inhibitors is disclosed. Guided by X-ray crystallographic data, optimization of an HTS lead led to the discovery of a series of 2-aryl, (N8)-alkyl substituted-6-aminosubstituted pyrido[3,2b]pyrazinones which s
Autor:
Richard B. Dorshow, Karen L. Wooley, Tim A. Marzan, Nam S. Lee, William L. Neumann, John N. Freskos, Jeng J. Shieh
Publikováno v:
Advanced Materials. 21:1344-1348
A pH-insensitive fluorophore is made to give pH-driven responses through its covalent incorporation within a nanostructure derived from pH-responsive polymers. Fluorophore-shell-crosslinked nanoparticles (SCKs) demonstrate notable enhancement of phot
Autor:
John N. Freskos, Yvette M. Fobian, Timothy E. Benson, Michael J. Bienkowski, David L. Brown, Thomas L. Emmons, Robert Heintz, Alice Laborde, Joseph J. McDonald, Brent V. Mischke, John M. Molyneaux, Joseph B. Moon, Patrick B. Mullins, D. Bryan Prince, Donna J. Paddock, Alfredo G. Tomasselli, Gregory Winterrowd
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:73-77
We describe a novel series of potent inhibitors of human beta-secretase. These compounds possess the hydroxyethyl amine transition state isostere. A 2.5A crystal structure of inhibitor 32 bound to BACE is provided.
Autor:
James R. Kiefer, Barta Thomas E, Heintz Robert M, Yvette M. Fobian, Daniel P. Becker, Grace E. Munie, Patrick B. Mullins, John M. Molyneaux, Brent V. Mischke, Darren J. Kassab, Louis J. Bedell, John N. Freskos
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:2823-2825
Continuing our interest in designing compounds preferentially potent and selective for MMP-13, we report on a series of hydroxamic acids with a flexible amide P1' substituents. We identify an amide which spares both MMP-1 and -14, and shows >500 fold
Autor:
Patrick B. Mullins, Huey-Sheng Shieh, John N. Freskos, Anna M. Stevens, Roderick A. Stegeman, Joseph J. McDonald, Mischke Brent
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 9:1757-1760
We have discovered a new series of potent conformationally constrained MMP Inhibitors that are selective for MMP-13 over MMP-1.