Zobrazeno 1 - 10
of 24
pro vyhledávání: '"Gunawardana Indrani W"'
Autor:
Darin Smith, Guy Vigers, Sumeet Rana, Michael Burkard, April Cox, Robert D. Groneberg, Ryan J. Watts, Robert Kirk Delisle, Tony Pisal Tang, Andrew T. Metcalf, Kelly Regal, Susan P. Rhodes, Mary K. Geck Do, Karin D. Brown, Joseph P. Lyssikatos, Douglas Mccord Sammond, Matthew Volgraf, Albion D. Wright, Gunawardana Indrani W, Kimberly Scearce-Levie, Jennifer N. Otten, Allen A. Thomas, Michael Siu, Hans E. Purkey, Kevin W. Hunt, Xingrong Liu, Darrin Dutcher
Publikováno v:
Journal of Medicinal Chemistry. 57:878-902
In an attempt to increase selectivity vs Cathepsin D (CatD) in our BACE1 program, a series of 1,3,4,4a,10,10a-hexahydropyrano[4,3-b]chromene analogues was developed. Three different Asp-binding moieties were examined: spirocyclic acyl guanidines, ami
Autor:
Barb Brandhuber, Stephen S. Gonzales, Guy Vigers, Kevin Ronald Condroski, Jed Pheneger, Patrice Lee, Allen A. Thomas, Y. Le Huerou, J. De Meese, Robin Pedersen, Jie Lin, Todd Romoff, Greg Poch, Christine Lemieux, Gunawardana Indrani W, Boyd Steven A, May Han, Francis X. Sullivan, Darin Smith, Bryan Bernat, Tomas Kaplan, Walter E. DeWolf, Josh Ballard, S. Kirk Wright, Solly Weiler
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:2206-2210
Tumor cells extensively utilize the pentose phosphate pathway for the synthesis of ribose. Transketolase is a key enzyme in this pathway and has been suggested as a target for inhibition in the treatment of cancer. In a pharmacodynamic study, nude mi
Autor:
Allen A. Thomas, Todd Romoff, Laura Hayter, Jed Pheneger, Jason De Meese, Patrice Lee, Boyd Steven A, S. Kirk Wright, Christine Lemieux, Gunawardana Indrani W, Steven S. Gonzales, Walter E. DeWolf, Francis X. Sullivan, Yvan Le Huerou, Jie Lin, Gregory K. Poch, May Han, Tomas Kaplan, Solly Weiler
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:505-508
Transketolase, a key enzyme in the pentose phosphate pathway, has been suggested as a target for inhibition in the treatment of cancer. Compound 5a ('N3'-pyridyl thiamine'; 3-(6-methyl-2-amino-pyridin-3-ylmethyl)-5-(2-hydroxy-ethyl)-4-methyl-thiazol-
Publikováno v:
Journal of Heterocyclic Chemistry. 45:91-96
Treatment of 3,5-dibromo- or 3,5-dichloro-pyridine-4-carboxaldehyde 2 with one equivalent of methyl thioglycolate, followed by exposure to base, provided 4-bromo- or 4-chloro-thieno[2,3-c]pyridine-2-carboxylate 4 in good yields. Oxidation of the thie
Autor:
Hunt, Kevin W., Cook, Adam W., Watts, Ryan J., Clark, Christopher T., Vigers, Guy, Smith, Darin, Metcalf, Andrew T., Gunawardana, Indrani W., Burkard, Michael, Cox, April A., Geck Do, Mary K., Dutcher, Darrin, Thomas, Allen A., Rana, Sumeet, Kallan, Nicholas C., DeLisle, Robert K., Rizzi, James P., Regal, Kelly, Sammond, Douglas, Groneberg, Robert, Siu, Michael, Purkey, Hans, Lyssikatos, Joseph P., Marlow, Allison, Liu, Xingrong, Tang, Tony P.
Publikováno v:
Journal of Medicinal Chemistry; 20240101, Issue: Preprints
Autor:
Akiyo Claiborne, Gang Liu, David Frost, Ken Jarvis, Jeffery D. Alder, Thomas W. von Geldern, and Qun Li, Joy Bauch, Laura Gehrke, William J. Chiou, Gunawardana Indrani W, Saul H. Rosenberg, Andrew Tasker, Jae Hwan-Soo, Bruce G. Szczepankiewicz, R. Bruce Credo, Yu Hua Hui, Michael A. Nukkala, Nicolette A. Zielinski, J. Ruth Wu-Wong, Stephen L. Gwaltney, Karl W. Mollison
Publikováno v:
Journal of Medicinal Chemistry. 44:4416-4430
During a screen for compounds that could inhibit cell proliferation, a series of new tubulin-binding compounds was identified with the discovery of oxadiazoline 1 (A-105972). This compound showed good cytotoxic activity against non-multi-drug-resista
Autor:
Andrew T. Metcalf, Allison Marlow, Robert Kirk Delisle, Ryan J. Watts, April Cox, Christopher T. Clark, Kelly Regal, Douglas Mccord Sammond, Kevin W. Hunt, Mary K. Geck Do, Guy Vigers, Sumeet Rana, James P. Rizzi, Tony Pisal Tang, Allen A. Thomas, Nicholas C. Kallan, Xingrong Liu, Adam W. Cook, Michael Siu, Darin Smith, Hans E. Purkey, Gunawardana Indrani W, Darrin Dutcher, Joseph P. Lyssikatos, Michael Burkard, Robert D. Groneberg
Publikováno v:
Journal of medicinal chemistry. 56(8)
A hallmark of Alzheimer's disease is the brain deposition of amyloid beta (Aβ), a peptide of 36-43 amino acids that is likely a primary driver of neurodegeneration. Aβ is produced by the sequential cleavage of APP by BACE1 and γ-secretase; therefo
Autor:
Jay R. Luly, Gunawardana Indrani W, Benjamin C. Lane, Gin C. Hsieh, Karl W. Mollison, Megumi Kawai
Publikováno v:
ChemInform. 29
Ascomycin 2, a close analogue of the immunosuppressant FK506 1, was modified to incorporate a hydroxyl group at the C-33 position. This increased the aqueous solubility of ascomycin by a hundred-fold at pH 7.4 and by approximately 300-fold at pH 6.5.
Publikováno v:
ChemInform. 39
Treatment of 3,5-dibromo- or 3,5-dichloro-pyridine-4-carboxaldehyde 2 with one equivalent of methyl thioglycolate, followed by exposure to base, provided 4-bromo- or 4-chloro-thieno[2,3-c]pyridine-2-carboxylate 4 in good yields. Oxidation of the thie
Autor:
Francis X. Sullivan, J. De Meese, Tomas Kaplan, Steven S. Gonzales, Josh Ballard, Solly Weiler, Joseph P. Lyssikatos, Thomas Daniel Aicher, Christine Lemieux, S. Kirk Wright, Barb Brandhuber, Gunawardana Indrani W, Allen A. Thomas, Todd Romoff, May Han, Kevin Ronald Condroski, Guy Vigers, Darin Smith, Bryan Bernat, Boyd Steven A, Y. Le Huerou, Walter E. DeWolf
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(2)
Inhibition of the thiamine-utilizing enzyme transketolase (TK) has been linked with diminished tumor cell proliferation. Most thiamine antagonists have a permanent positive charge on the B-ring, and it has been suggested that this charge is required