Zobrazeno 1 - 10
of 11
pro vyhledávání: '"George Diamantidis"'
Autor:
Nancy Torres, Eileen Frommer, Bloom Jonathan David, Karen Collins, Dunnick Alejandro Lee, George Diamantidis, Yongbo Hu, Minu Dutia, Christoph W. Zapf, Zhang Chunchun, Darrin William Hopper, Dan Maarten Berger, Donald Wojciechowicz, Dennis Powell, Martin Di Grandi, Jeremy I. Levin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:6957-6961
A novel series of pyrazolo[1,5-a]pyrimidines bearing a 3-hydroxyphenyl group at C(3) and substituted tropanes at C(7) have been identified as potent B-Raf inhibitors. Exploration of alternative functional groups as a replacement for the C(3) phenol d
Autor:
Karen L. Marquis, Suzan Aschmies, Hua Zhou, Robert Martone, Kevin Atchison, June Sonnenberg-Reines, Anthony Kreft, Menelas N. Pangalos, Thomas A. Comery, J. Steven Jacobsen, George Diamantidis, Xiaohai Gong
Publikováno v:
The Journal of Neuroscience. 25:8898-8902
Transgenic mice (Tg2576) overexpressing the Swedish mutation of the human amyloid precursor protein display biochemical, pathological, and behavioral markers consistent with many aspects of Alzheimer's disease, including impaired hippocampal function
Autor:
Stacy W. Remiszewski, Lidia C. Sambucetti, Kenneth W. Bair, John Bontempo, David Cesarz, Nagarajan Chandramouli, Ru Chen, Min Cheung, Susan Cornell-Kennon, Karl Dean, George Diamantidis, Dennis France, Michael A. Green, Kobporn Lulu Howell, Rina Kashi, Paul Kwon, Peter Lassota, Mary S. Martin, Yin Mou, Lawrence B. Perez, Sushil Sharma, Troy Smith, Eric Sorensen, Francis Taplin, Nancy Trogani, Richard Versace, Heather Walker, Susan Weltchek-Engler, Alexander Wood, Arthur Wu, Peter Atadja
Publikováno v:
Journal of Medicinal Chemistry. 46:4609-4624
A series of N-hydroxy-3-phenyl-2-propenamides were prepared as novel inhibitors of human histone deacetylase (HDAC). These compounds were potent enzyme inhibitors, having IC50s < 400 nM in a partially purified enzyme assay. However, potency in cell g
Autor:
Boyd L. Harrison, Dennis Kubrak, Kimberly Sogi, George Diamantidis, Anthony F. Kreft, Zheng Wang, Zhang Minsheng, Scott Christian Mayer, Lynn Resnick, Alex Porte
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:2401-2403
An asymmetric synthesis of alpha-amino acids with novel beta-branched side chains has been implemented. The syntheses feature a p-toluenesulfinylimine induced chiral Strecker approach and were found to be applicable to the introduction of both alipha
Autor:
Hong Fan, T. R. Wagler, K. Natalie, Ramachandran S. Ranganathan, Thangavel Arunachalam, N. Soundararajan, George Diamantidis, C.-K. Chen, K. M. R. Pillai, Edmund R. Marinelli, R. Neubeck, J. Emswiler
Publikováno v:
ChemInform. 28
Autor:
Joshua D Berkowitz, Boyd L. Harrison, Robert Martone, Hua Zhou, Micheal Chlenov, Yun Hu, Peimin Lu, Koi Michele Morris, June Sonnenberg-Reines, S. Aschmies, Joan E. Sabalski, Kerri Lipinski, George Diamantidis, Kevin Atchison, Thomas J. Caggiano, Shaiu-Ching Sun, Zheng Xu, Jun Pu, Anthony F. Kreft, Dave R. Riddell, Yiqun Wang, Lynn Resnick, Mei Jin, Donna M. Huryn, Erik Wagner, J. Steven Jacobsen
Publikováno v:
Bioorganicmedicinal chemistry. 17(13)
gamma-Secretase inhibitors have been shown to reduce the production of beta-amyloid, a component of the plaques that are found in brains of patients with Alzheimer's disease. A novel series of heterocyclic sulfonamide gamma-secretase inhibitors that
Autor:
Ron Magolda, Joseph R. Stock, David Riddell, Scott C. Mayer, John Ellingboe, Ting Wang, Melissa Lin, Hua Zhou, Yun Hu, Galante Rocco, Dennis M. Kubrak, Mei Jin, Madelene Miyoko Antane, Aram Oganesian, Anthony Kreft, Margaret M. Zaleska, Derek C. Cole, Michael Chlenov, Minsheng Zhang, Menelas N. Pangalos, Alex M. Porte, J. Steven Jacobsen, Lynn Resnick, Joseph Zeldis, Kristi Fan, Donna M. Huryn, Uday Jain, Shaiu-Ching Sun, Cathleen Gonzales, Boyd L. Harrison, William E. Moore, Peimin Lu, Magid Abou-Gharbia, Thomas A. Comery, Molly Hoke, Suzan Aschmies, George Diamantidis, Kevin R. Woller, Peter H. Reinhart, Robert Martone, June Sonnenberg-Reines, Kevin Atchison, Erik Wagner, Zheng Xu, Douglas M. Ho, Kenneth Alfred Martin Kremer
Publikováno v:
Journal of medicinal chemistry. 51(23)
SAR on HTS hits 1 and 2 led to the potent, Notch-1-sparing GSI 9, which lowered brain Abeta in Tg2576 mice at 100 mg/kg po. Converting the metabolically labile methyl groups in 9 to trifluoromethyl groups afforded the more stable analogue 10, which h
Autor:
Peimin Lu, David S. Casebier, Dennis Kubrak, S. Aschmies, David Riddell, William Jay Moore, Zheng Wang, Mei Jin, Hua Zhou, Thomas A. Comery, John W. Ellingboe, Shaiu-Ching Sun, Erik Wagner, Aram Oganesian, Joseph Raymond Stock, Boyd L. Harrison, Zheng Xu, Robert Martone, George Diamantidis, Madelene Antane, Kevin Atchison, Kevin R. Woller, Yun Hu, June Sonnenberg-Reines, Charles William Mann, J. Steven Jacobsen, Anthony F. Kreft, Derek C. Cole
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(3)
Accumulation of beta-amyloid (Abeta), produced by the proteolytic cleavage of amyloid precursor protein (APP) by beta- and gamma-secretase, is widely believed to be associated with Alzheimer's disease (AD). Research around the high-throughput screeni
Autor:
Magid Abou-Gharbia, Anthony Kreft, Peter H. Reinhart, J. Steven Jacobsen, Kevin Atchison, Robert Martone, Scott C. Mayer, Lynn Resnick, Ronald L. Magolda, Menelas N. Pangalos, Dennis M. Kubrak, Boyd L. Harrison, Kerri Lipinski, Ann Aulabaugh, Warren D. Hirst, Hua Zhou, Xinyi Huang, Michael K. May, Alex M. Porte, George Diamantidis
Publikováno v:
Alzheimer's & Dementia. 4
Autor:
Hua Zhou, John W. Ellingboe, Derek Cecil Cole, Donna M. Huryn, Suzan Aschmies, Mei Jin, Charles William Mann, William E. Moore, Robert Martone, David S. Casebier, George Diamantidis, Zheng Xu, Alex Porte, Kevin R. Woller, Kevin Atchison, Anthony F. Kreft, Erik Wagner, Yun Hu, June Sonnenberg-Reines, Joseph T. Lundquist, J. Steven Jacobsen, Dennis Kubrak, Dave R. Riddell, Peimin Lu, Diane B. Hauze, Joseph Raymond Stock, Shaiu-Ching Sun, Boyd L. Harrison, Aram Oganesian
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(14)
Using a cell-based assay, we have identified a new series of Notch-sparing gamma-secretase inhibitors from HTS screening leads 2a and 2e. Lead optimization studies led to the discovery of analog 8e with improved gamma-secretase inhibitory potency and