Search Results - "Smalley, Terrence L"

Discovery, Synthesis, and Biological Evaluation of Thiazoloquin(az)olin(on)es as Potent CD38 Inhibitors by Haffner, Curt D, Becherer, J. David, Boros, Eric E, Cadilla, Rodolfo, Carpenter, Tiffany, Cowan, David, Deaton, David N, Guo, Yu, Harrington, Wallace, Henke, Brad R, Jeune, Michael R, Kaldor, Istvan, Milliken, Naphtali, Petrov, Kim G, Preugschat, Frank, Schulte, Christie, Shearer, Barry G, Shearer, Todd, Smalley, Terrence L, Stewart, Eugene L, Stuart, J. Darren, Ulrich, John C

“…A series of thiazoloquin­(az)­olinones were synthesized and found to have potent inhibitory activity against CD38. Several of these compounds were also shown…”
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Novel heterocyclic scaffolds of GW4064 as farnesoid X receptor agonists by Smalley, Jr, Terrence L, Boggs, Sharon, Caravella, Justin A, Chen, Lihong, Creech, Katrina L, Deaton, David N, Kaldor, Istvan, Parks, Derek J

“…The farnesoid X receptor (FXR) may play a crucial role in a number of metabolic diseases and, as such, could potentially serve as a target for the development…”
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Unique Cellular and Biochemical Features of Human Mitochondrial Peroxiredoxin 3 Establish the Molecular Basis for Its Specific Reaction with Thiostrepton by Nelson, Kimberly J, Messier, Terri, Milczarek, Stephanie, Saaman, Alexis, Beuschel, Stacie, Gandhi, Uma, Heintz, Nicholas, Smalley, Terrence L, Lowther, W Todd, Cunniff, Brian

“…A central hallmark of tumorigenesis is metabolic alterations that increase mitochondrial reactive oxygen species (mROS). In response, cancer cells upregulate…”
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Conformationally constrained farnesoid X receptor (FXR) agonists: Heteroaryl replacements of the naphthalene by Bass, Jonathan Y., Caravella, Justin A., Chen, Lihong, Creech, Katrina L., Deaton, David N., Madauss, Kevin P., Marr, Harry B., McFadyen, Robert B., Miller, Aaron B., Mills, Wendy Y., Navas, Frank, Parks, Derek J., Smalley, Terrence L., Spearing, Paul K., Todd, Dan, Williams, Shawn P., Wisely, G. Bruce

“…To improve on the drug properties of GSK8062 1b, a series of heteroaryl bicyclic naphthalene replacements were prepared. The quinoline 1c was an equipotent FXR…”
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Discovery of 4‑Amino-8-quinoline Carboxamides as Novel, Submicromolar Inhibitors of NAD-Hydrolyzing Enzyme CD38 by Becherer, J. David, Boros, Eric E., Carpenter, Tiffany Y., Cowan, David J., Deaton, David N., Haffner, Curt D., Jeune, Michael R., Kaldor, Istvan W., Poole, J. Chuck, Preugschat, Frank, Rheault, Tara R., Schulte, Christie A., Shearer, Barry G., Shearer, Todd W., Shewchuk, Lisa M., Smalley, Terrence L., Stewart, Eugene L., Stuart, J. Darren, Ulrich, John C.

“…Starting from the micromolar 8-quinoline carboxamide high-throughput screening hit 1a, a systematic exploration of the structure–activity relationships (SAR)…”
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A knowledge-based, structural-aided discovery of a novel class of 2-phenylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors by Schulte, Christie A., Deaton, David N., Diaz, Elsie, Do, Young, Gampe, Robert T., Guss, Jeffrey H., Hancock, Ashley P., Hobbs, Heather, Hodgson, Simon T., Holt, Jason, Jeune, Michael R., Kahler, Kirsten M., Kramer, H. Fritz, Le, Joelle, Mortenson, Paul N., Musetti, Caterina, Nolte, Robert T., Orband-Miller, Lisa A., Peckham, Gregory E., Petrov, Kim G., Pietrak, Beth L., Poole, Chuck, Price, Daniel J., Saxty, Gordon, Shillings, Anthony, Smalley, Terrence L., Somers, Don O., Stewart, Eugene L., Stuart, J. Darren, Thomson, Stephen A.

“…Through an internal virtual screen performed at GlaxoSmithKline a distinct class of 2-phenylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors were…”
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Synthesis and activity of small molecule GPR40 agonists by Garrido, Dulce M., Corbett, David F., Dwornik, Kate A., Goetz, Aaron S., Littleton, Thomas R., McKeown, Steve C., Mills, Wendy Y., Smalley, Terrence L., Briscoe, Celia P., Peat, Andrew J.

“…The first report on the identification and structure–activity relationships of a novel series of GPR40 agonists based on a 3-(4-{[…”
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Synthesis and evaluation of novel heterocyclic inhibitors of GSK-3 by Smalley, Terrence L., Peat, Andrew J., Boucheron, Joyce A., Dickerson, Scott, Garrido, Dulce, Preugschat, Frank, Schweiker, Stephanie L., Thomson, Stephen A., Wang, Tony Y.

“…Novel heterocyclic GSK-3 inhibitors based on a previously described template have been synthesized as a potential treatment for diabetes. Several compounds…”
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Synthesis of novel anilinoquinolines as c-fms inhibitors by Smalley, Terrence L., Chamberlain, Stanley D., Mills, Wendy Y., Musso, David L., Randhawa, Sab A., Ray, John A., Samano, Vicente, Frick, Lloyd

“…A novel series of potent substituted anilinoquinolines were discovered as c-fms inhibitors. The potency could be manipulated upon modification of the C4…”
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Total Synthesis of (±)-Isostemofoline by Kende, Andrew S, Smalley, Terrence L, Huang, He

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Synthesis of Cobalt Substituted 1,3-Diene Complexes with Unusual Structures and Their Exo Selective Diels-Alder Reactions by Wright, Marcus W, Smalley, Terrence L, Welker, Mark E, Rheingold, Arnold L

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Regioselective synthesis of 3,3-diethyl-4-(methylene)-1-quinol-2-ones by an intramolecular microwave assisted heck reaction by Smalley Jr, Terrence L., Mills, Wendy Y.

“…A protocol for the intramolecular Heck cyclization to afford 3,3‐diethyl‐4‐(methylene)‐1‐quinol‐2‐ones is described. We observed that the use of microwave…”
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Synthesis of 2-transition-metal-substituted 1,3-butadienyl complexes with unusual structures and facile Diels-Alder reactions of cobalt 1,3-butadiene complexes by Smalley, Terrence L, Wright, Marcus W, Garmon, Stuart A, Welker, Mark E, Rheingold, Arnold L

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A synthetic approach to stemofoline: The total synthesis of (+/1)-isostemofoline by Smalley, Terrence L., Jr

“…A synthetic approach to the hexacyclic alkaloid stemofoline (1 ) is discussed. The total synthesis of (+/-)-isostemofoline (145) was completed in 24 steps. The…”
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A Ring Expansion Strategy in Antiviral Synthesis: A Novel Approach to TAK-779 by Smalley, Terrence L.

“…A synthesis of TAK-779 that relies on construction of a key carboxylic acid intermediate by a ring expansion with TMSCHN 2 is described…”
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Substrate Specificity in Short-Chain Phospholipid Analogs at the Active Site of Human Synovial Phospholipase A2 by Wheeler, T. N, Blanchard, Steven G, Fang, Frank, Gray-Nunez, Yolanda, Harris, Cole O, Lambert, Millard H, Mehrotra, Mukund M, Parks, Derek J, Andrew, R. C

“…The substrate specificity at the active site of recombinant human synovial fluid phospholipase A2 (hs-PLA2) was investigated by the preparation of a series of…”
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