Search Results - "GEE-HONG KUO"

Synthesis and Biological Evaluation of 3-Aryl-3-(4-phenoxy)-propionic Acid as a Novel Series of G Protein-Coupled Receptor 40 Agonists by Song, Fengbin, Lu, Songfeng, Gunnet, Joe, Xu, Jun Z, Wines, Pam, Proost, Jef, Liang, Yin, Baumann, Chris, Lenhard, Jim, Murray, William V, Demarest, Keith T, Kuo, Gee-Hong

“…High-throughput screening of a subset of the J&J compound library containing the carboxylic acid functional group uncovered a bromophenyl derivative as a…”
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Synthesis and Identification of [1,3,5]Triazine-pyridine Biheteroaryl as a Novel Series of Potent Cyclin-Dependent Kinase Inhibitors by Kuo, Gee-Hong, DeAngelis, Alan, Emanuel, Stuart, Wang, Aihua, Zhang, Yan, Connolly, Peter J, Chen, Xin, Gruninger, Robert H, Rugg, Catherine, Fuentes-Pesquera, Angel, Middleton, Steven A, Jolliffe, Linda, Murray, William V

“…On the basis of previous studies, we identified pyrazine-pyridine A as a potent vascular endothelial growth factor inhibitor and pyrimidine-pyridine B as a…”
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5,5-Difluoro- and 5-Fluoro-5-methyl-hexose-based C-Glucosides as potent and orally bioavailable SGLT1 and SGLT2 dual inhibitors by Xu, Guozhang, Du, Fuyong, Kuo, Gee-Hong, Xu, June Zhi, Liang, Yin, Demarest, Keith, Gaul, Michael D.

“…[Display omitted] (2S,3R,4R,5S,6R)-2-Aryl-5,5-difluoro-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4-diols and…”
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An efficient and scalable synthesis of (2R,αS)-3,4-dihydro-2-[3-(1,1,2,2-tetrafluoroethoxy)phenyl]-5-[3-(trifluoromethoxy)phenyl]-α-(trifluoromethyl)-1(2H)-quinolineethanol: A potent CETP inhibitor by Wang, Aihua, Zhang, Yan, Lu, Songfeng, Murray, William V., Kuo, Gee-Hong

“…An efficient and scalable synthesis of the potent CETP inhibitor,…”
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Synthesis and biological evaluation of benzocyclobutane-C-glycosides as potent and orally active SGLT1/SGLT2 dual inhibitors by Kuo, Gee-Hong, Gaul, Micheal D., Liang, Yin, Xu, June Z., Du, Fuyong, Hornby, Pamela, Xu, Guozhang, Qi, Jenson, Wallace, Nathaniel, Lee, Seunghun, Grant, Eugene, Murray, William V., Demarest, Keith

“…[Display omitted] Synthesis and biological evaluation of benzocyclobutane-C-glycosides as potent and orally active SGLT1/SGLT2 dual inhibitors are described…”
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Design, synthesis and biological evaluation of (2S,3R,4R,5S,6R)-5-fluoro-6-(hydroxymethyl)-2-aryltetrahydro-2H-pyran-3,4-diols as potent and orally active SGLT dual inhibitors by Xu, Guozhang, Gaul, Michael D., Kuo, Gee-Hong, Du, Fuyong, Xu, June Zhi, Wallace, Nathaniel, Hinke, Simon, Kirchner, Thomas, Silva, Jose, Huebert, Norman D., Lee, Seunghun, Murray, William, Liang, Yin, Demarest, Keith

“…[Display omitted] •A new series of SGLT1 and SGLT2 dual inhibitors were disclosed.•Two methods were developed to efficiently synthesize C5-fluoro-lactones 3…”
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Synthesis of β‑Substituted Cyclic Enones via Phosphonium Salt-Activated, Palladium-Catalyzed Cross-Coupling of Cyclic 1,3-Diones by Yang, Shyh-Ming, Kuo, Gee-Hong, Gaul, Michael D, Murray, William V

“…Phosphonium salt-activated, Pd-catalyzed Suzuki–Miyaura and Sonogashira cross-coupling reactions of cyclic 1,3-diones in the synthesis of β-substituted cyclic…”
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Design and synthesis of potent inhibitors of cholesteryl ester transfer protein (CETP) exploiting a 1,2,3,4-tetrahydroquinoline platform by Rano, Thomas A., Sieber-McMaster, Ellen, Pelton, Patricia D., Yang, Maria, Demarest, Keith T., Kuo, Gee-Hong

“…Tetrahydroquinoline A is a potent inhibitor of the cholesterol ester transfer protein (CETP), a target for the treatment of low HDL-C and atherosclerosis…”
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Improved Asymmetric Synthesis of 3,4-Dihydro-2-[3-(1,1,2,2-tetrafluoroethoxy)phenyl]-5-[3-(trifluoromethoxy)phenyl]-α-(trifluoromethyl)-1(2H)-quinolineethanol, a Potent Cholesteryl Ester Transfer Protein Inhibitor by Rano, Thomas A, Kuo, Gee-Hong

“…The asymmetric synthesis of 3,4-dihydro-2-[3-(1,1,2,2-tetrafluoroethoxy)phenyl]-5-[3-(trifluoromethoxy)phenyl]-α-(trifluoromethyl)-1(2H)-quinolineethanol…”
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Metabolic tracing of monoacylglycerol acyltransferase-2 activity in vitro and in vivo by Qi, Jenson, Lang, Wensheng, Connelly, Margery A, Du, Fuyong, Liang, Yin, Caldwell, Gary W, Martin, Tonya, Hansen, Michael K, Kuo, Gee-Hong, Gaul, Michael D, Pocai, Alessandro, Lee, Seunghun

“…Monoacylglycerol acyltransferase 2 (MGAT2) catalyzes the synthesis of diacylglycerol (DAG) from free fatty acids (FFA) and sn-monoacylglycerol (MG), the two…”
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Synthesis and discovery of 2,3-dihydro-3,8-diphenylbenzo[1,4]oxazines as a novel class of potent cholesteryl ester transfer protein inhibitors by Wang, Aihua, Prouty, Catherine P., Pelton, Patricia D., Yong, Maria, Demarest, Keith T., Murray, William V., Kuo, Gee-Hong

“…2,3-Dihydro-3,8-diphenylbenzo[1,4]oxazine 6a is a potent inhibitor (IC 50 = 26 nM) of cholesteryl ester transfer protein (CETP). It possesses a favorable…”
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Optimization of a pyrazole hit from FBDD into a novel series of indazoles as ketohexokinase inhibitors by Zhang, Xuqing, Song, Fengbing, Kuo, Gee-Hong, Xiang, Amy, Gibbs, Alan C., Abad, Marta C., Sun, Weimei, Kuo, Lawrence C., Sui, Zhihua

“…A series of indazoles have been discovered as KHK inhibitors from a pyrazole hit identified through fragment based drug discovery. The lead compounds showed…”
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4-Bicyclic heteroaryl-piperidine derivatives as potent, orally bioavailable stearoyl-CoA desaturase-1 (SCD1) inhibitors: part 2. Pyridazine-based analogs by Yang, Shyh-Ming, Tang, Yuting, Rano, Thomas, Lu, Huajun, Kuo, Gee-Hong, Gaul, Michael D, Li, Yaxin, Ho, George, Lang, Wensheng, Conway, James G, Liang, Yin, Lenhard, James M, Demarest, Keith T, Murray, William V

“…Design, synthesis, and biological evaluation of pyridazine-based, 4-bicyclic heteroaryl-piperidine derivatives as potent stearoyl-CoA desaturase-1 (SCD1)…”
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3-(7-Azaindolyl)-4-arylmaleimides as potent, selective inhibitors of glycogen synthase kinase-3 by Zhang, Han-Cheng, Ye, Hong, Conway, Bruce R., Derian, Claudia K., Addo, Michael F., Kuo, Gee-Hong, Hecker, Leonard R., Croll, Diane R., Li, Jian, Westover, Lori, Xu, Jun Z., Look, Richard, Demarest, Keith T., Andrade-Gordon, Patricia, Damiano, Bruce P., Maryanoff, Bruce E.

“…A novel series of 3-(7-azaindolyl)-4-(aryl/heteroaryl)maleimides was identified as potent GSK-3β inhibitors with excellent selectivity over PKC-βII…”
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4-Bicyclic heteroaryl-piperidine derivatives as potent, orally bioavailable Stearoyl-CoA desaturase-1 (SCD1) inhibitors. Part 1: Urea-based analogs by Yang, Shyh-Ming, Tang, Yuting, Zhang, Rui, Lu, Huajun, Kuo, Gee-Hong, Gaul, Michael D., Li, Yaxin, Ho, George, Conway, James G., Liang, Yin, Lenhard, James M., Demarest, Keith T., Murray, William V.

“…A new series of urea-based, 4-bicyclic heteroaryl-piperidine derivatives as potent SCD1 inhibitors is described. The structure–activity relationships focused…”
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Torcetrapib Produces Endothelial Dysfunction Independent of Cholesteryl Ester Transfer Protein Inhibition by Connelly, Margery A, Parry, Tom J, Giardino, Edward C, Huang, Zhihong, Cheung, Wai-man, Chen, Cailin, Cools, Frank, Van der Linde, Henk, Gallacher, David J, Kuo, Gee-Hong, Sarich, Troy C, Demarest, Keith T, Damiano, Bruce P

“…OBJECTIVE:Torcetrapib, a prototype cholesteryl ester transfer protein (CETP) inhibitor with potential for decreasing atherosclerotic disease, increased…”
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Synthesis and Identification of [1,2,4]Thiadiazole Derivatives as a New Series of Potent and Orally Active Dual Agonists of Peroxisome Proliferator-Activated Receptors α and δ by Shen, Lan, Zhang, Yan, Wang, Aihua, Sieber-McMaster, Ellen, Chen, Xiaoli, Pelton, Patricia, Xu, Jun Z, Yang, Maria, Zhu, Peifang, Zhou, Lubing, Reuman, Michael, Hu, Zhiyong, Russell, Ronald, Gibbs, Alan C, Ross, Hamish, Demarest, Keith, Murray, William V, Kuo, Gee-Hong

“…Cardiovascular disease is the most common cause of morbidity and mortality in developed nations. To effectively target dyslipidemia to reduce the risk of…”
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Synthesis and Discovery of Macrocyclic Polyoxygenated Bis-7-azaindolylmaleimides as a Novel Series of Potent and Highly Selective Glycogen Synthase Kinase-3β Inhibitors by Kuo, Gee-Hong, Prouty, Catherine, DeAngelis, Alan, Shen, Lan, O'Neill, David J, Shah, Chandra, Connolly, Peter J, Murray, William V, Conway, Bruce R, Cheung, Peter, Westover, Lori, Xu, Jun Z, Look, Richard A, Demarest, Keith T, Emanuel, Stuart, Middleton, Steven A, Jolliffe, Linda, Beavers, Mary Pat, Chen, Xin

“…Attempts to design the macrocyclic maleimides as selective protein kinase C γ inhibitors led to the unexpected discovery of a novel series of potent and highly…”
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Novel LC/MS/MS and High-Throughput Mass Spectrometric Assays for Monoacylglycerol Acyltransferase Inhibitors by Qi, Jenson, Masucci, John A, Lang, Wensheng, Connelly, Margery A, Caldwell, Gary W, Petrounia, Ioanna, Kirkpatrick, Jennifer, Barnakov, Alexander N, Struble, Geoffrey, Miller, Robyn, Dzordzorine, Keli, Kuo, Gee-Hong, Gaul, Michael, Pocai, Alessandro, Lee, Seunghun

“…Monoacylglycerol acyltransferase enzymes (MGAT1, MGAT2, and MGAT3) convert monoacylglycerol to diacylglycerol (DAG). MGAT1 and MGAT2 are both implicated in…”
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Discovery and SAR of para-alkylthiophenoxyacetic acids as potent and selective PPARδ agonists by Zhang, Rui, DeAngelis, Alan, Wang, Aihua, Sieber-McMaster, Ellen, Li, Xun, Russell, Ronald, Pelton, Patricia, Xu, Jun, Zhu, Peifang, Zhou, Lubing, Demarest, Keith, Murray, William V., Kuo, Gee-Hong

“…Synthesis and SAR of potent and selective PPARδ agonists is described. Synthesis and SAR of para-alkylthiophenoxyacetic acids is described. Achiral compounds…”
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