MichaelHing-WahSiuMDAAFM

PubMed

• 15 citations
  Discovery of a class of highly potent Janus Kinase 1/2 (JAK1/2) inhibitors demonstrating effective cell-based blockade of IL-13 signaling.
  Mark Zak, Emily J. Hanan, Patrick J. Lupardus, D.G. Brown, C. Robinson, Michael Siu, Joseph P. Lyssikatos, F.A. Romero, Guiling Zhao, Terry Kellar, Rohan Mendonca, Nic...> ;Bioorganic & Medicinal Chemistry Letters. 2019 Jun 15
• 38 citations
  Scaffold-Hopping and Structure-Based Discovery of Potent, Selective, And Brain Penetrant N-(1H-Pyrazol-3-yl)pyridin-2-amine Inhibitors of Dual Leucine Zipper Kinase (D...
  Snahel Patel, Seth F. Harris, Paul Gibbons, Gauri Deshmukh, Amy Gustafson, Terry Kellar, Han Lin, Xingrong Liu, Yanzhou Liu, Yichin Liu, Changyou Ma, Kimberly Scearce-...> ;Journal of Medicinal Chemistry. 2015 Oct 2
• 60 citations
  Discovery of Dual Leucine Zipper Kinase (DLK, MAP3K12) Inhibitors with Activity in Neurodegeneration Models
  Snahel Patel, Frederick Cohen, Brian Dean, Kelly De La Torre, Gauri Deshmukh, Anthony A. Estrada, Arundhati Sengupta Ghosh, Paul Gibbons, Amy Gustafson, Malcolm P. Hue...> ;Journal of Medicinal Chemistry. 2015 Jan 8
• 11 citations
  8-Tetrahydropyran-2-yl chromans: highly selective beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors.
  Allen A. Thomas, Kevin W. Hunt, Brad Newhouse, Ryan J. Watts, Xingrong Liu, Guy Vigers, Darin Smith, Susan P. Rhodes, Karin D. Brown, Jennifer N. Otten, Michael Burkar...> ;Journal of Medicinal Chemistry. 2014 Nov 26
• 9 citations
  Synthesis, characterization, and PK/PD studies of a series of spirocyclic pyranochromene BACE1 inhibitors.
  Matthew Volgraf, Lina Chan, Malcolm P. Huestis, Hans E. Purkey, Michael Burkard, Mary Geck Do, Julie Harris, Kevin W. Hunt, Xingrong Liu, Joseph P. Lyssikatos, Sumeet ...> ;Bioorganic & Medicinal Chemistry Letters. 2014 Jun 1
• 24 citations
  Discovery of 7-tetrahydropyran-2-yl chromans: β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors that reduce amyloid β-protein (Aβ) in the central n...
  Allen A. Thomas, Kevin W. Hunt, Matthew Volgraf, Ryan J. Watts, Xingrong Liu, Guy Vigers, Darin Smith, Douglas Mccord Sammond, Tony Pisal Tang, Susan P. Rhodes, Andrew...> ;Journal of Medicinal Chemistry. 2014 Jan 22
• 23 citations
  2-Amino-[1,2,4]triazolo[1,5-a]pyridines as JAK2 inhibitors
  Michael Siu, Richard Pastor, Liu Wendy, Kathy Barrett, Megan Berry, Wade S. Blair, Christine Chang, Jacob Z. Chen, Charles Eigenbrot, Nico Ghilardi, Paul Gibbons, Haiy...> ;Bioorganic & Medicinal Chemistry Letters. 2013 Sep 1
• 43 citations
  Spirocyclic β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors: from hit to lowering of cerebrospinal fluid (CSF) amyloid β in a higher species.
  Kevin W. Hunt, Adam W. Cook, Ryan J. Watts, Christopher T. Clark, Guy Vigers, Darin Smith, Andrew T. Metcalf, Gunawardana Indrani W, Michael Burkard, April Cox, Mary K...> ;Journal of Medicinal Chemistry. 2013 Apr 16
• 8 citations
  N -(Pyridin-2-yl) arylsulfonamide inhibitors of 11β-hydroxysteroid dehydrogenase type 1: Strategies to eliminate reactive metabolites
  Sajiv Krishnan Nair, Jean Joo Matthews, Cripps Stephan James, Cheng Hengmiao, Jacqui Elizabeth Hoffman, Christopher Ronald Smith, Stanley William Kupchinsky, Michael S...> ;Bioorganic & Medicinal Chemistry Letters. 2013 Apr 15
• 47 citations
  Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors.
  Emily J. Hanan, Anne van Abbema, Kathy Barrett, Wade S. Blair, Jeffrey M. Blaney, Christine Chang, Charles Eigenbrot, Sean P. Flynn, Paul Gibbons, Christopher A. Hurle...> ;Journal of Medicinal Chemistry. 2012 Oct 24
• 18 citations
  Structure-based design of thienobenzoxepin inhibitors of PI3-kinase.
  Steven T. Staben, Michael Siu, Richard Goldsmith, Alan G. Olivero, Steven Do, Daniel J. Burdick, Timothy P. Heffron, Jenna Dotson, Daniel P. Sutherlin, Bing-Yan Zhu, V...> ;Bioorganic & Medicinal Chemistry Letters. 2011 Jul 1
• 34 citations
  N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275.
  Michael Siu, Theodore O. Johnson, Yong Wang, Sajiv Krishnan Nair, Taylor Wendy Dianne, Cripps Stephan James, Jean Joo Matthews, Martin Paul Edwards, Thomas A. Pauly, J...> ;Bioorganic & Medicinal Chemistry Letters. 2009 Jul 1
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