Search Results - "Georg, I"

The Ecstasy and Agony of Assay Interference Compounds by Aldrich, Courtney, Bertozzi, Carolyn, Georg, Gunda I, Kiessling, Laura, Lindsley, Craig, Liotta, Dennis, Merz, Jr, Kenneth M, Schepartz, Alanna, Wang, Shaomeng

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A preclinical evaluation of Minnelide as a therapeutic agent against pancreatic cancer by Chugh, Rohit, Sangwan, Veena, Patil, Satish P, Dudeja, Vikas, Dawra, Rajinder K, Banerjee, Sulagna, Schumacher, Robert J, Blazar, Bruce R, Georg, Gunda I, Vickers, Selwyn M, Saluja, Ashok K

“…Pancreatic cancer is one of the most lethal human malignancies with an all-stage 5-year survival frequency of <5%, which highlights the urgent need for more…”
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Synthesis of Amino Acid Derived Enaminones via Wolff Rearrangement Using Vinylogous Amides as Carbon Nucleophiles by Seki, Hajime, Georg, Gunda I

“…Cyclic enaminones were synthesized in high yields from amino acids in two steps via Wolff rearrangement. The cyclization represents a rare 6-exo-dig…”
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Boron–Heck Reaction of Cyclic Enaminones: Regioselective Direct Arylation via Oxidative Palladium(II) Catalysis by Kim, Yong Wook, Georg, Gunda I

“…An oxidative boron–Heck reaction of cyclic enaminones with arylboronic acids is reported. This protocol provides a regioselective arylation at the C6 position…”
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Palladium(II)-Catalyzed Direct Arylation of Enaminones Using Organotrifluoroborates by Ge, Haibo, Niphakis, Micah J, Georg, Gunda I

“…A Pd(II)-catalyzed reaction for the direct arylation of cyclic enaminones is reported. The reactivity of electron-rich, electron-poor, and sterically…”
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Development of allosteric and selective CDK2 inhibitors for contraception with negative cooperativity to cyclin binding by Faber, Erik B., Sun, Luxin, Tang, Jian, Roberts, Emily, Ganeshkumar, Sornakala, Wang, Nan, Rasmussen, Damien, Majumdar, Abir, Hirsch, Laura E., John, Kristen, Yang, An, Khalid, Hira, Hawkinson, Jon E., Levinson, Nicholas M., Chennathukuzhi, Vargheese, Harki, Daniel A., Schönbrunn, Ernst, Georg, Gunda I.

“…Compared to most ATP-site kinase inhibitors, small molecules that target an allosteric pocket have the potential for improved selectivity due to the often…”
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Synthesis of Tylocrebrine and Related Phenanthroindolizidines by VOF3-Mediated Oxidative Aryl-Alkene Coupling by Niphakis, Micah J, Georg, Gunda I

“…A highly convergent strategy to prepare phenanthroindolizidines is reported involving three consecutive C−C coupling reactions. This sequence features a novel…”
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Structural Basis of ALDH1A2 Inhibition by Irreversible and Reversible Small Molecule Inhibitors by Chen, Yan, Zhu, Jin-Yi, Hong, Kwon Ho, Mikles, David C, Georg, Gunda I, Goldstein, Alex S, Amory, John K, Schönbrunn, Ernst

“…Enzymes of the ALDH1A subfamily of aldehyde dehydrogenases are crucial in regulating retinoic acid (RA) signaling and have received attention as potential drug…”
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AAC services for multilingual populations: South African service provider perspectives by Tönsing, Kerstin M, van Niekerk, Karin, Schlünz, Georg I, Wilken, Ilana

“…•Service providers use mono- and multilingual approaches for clients in need of AAC.•Macro- and microlevel factors influence language choices in AAC…”
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A concise formal total synthesis of lactimidomycin by Li, Wei, Georg, Gunda I

“…A formal total synthesis of the cytotoxic natural product lactimidomycin has been achieved in nine steps from (E)-2-methyl-2-pentenoic acid. The 12-membered…”
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Mild and Selective Hydrozirconation of Amides to Aldehydes Using Cp2Zr(H)Cl:  Scope and Mechanistic Insight by Spletstoser, Jared T, White, Jonathan M, Tunoori, Ashok Rao, Georg, Gunda I

“…An investigation of the use of Cp2Zr(H)Cl (Schwartz's reagent) to reduce a variety of amides to the corresponding aldehydes under very mild reaction conditions…”
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Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts by Patil, Satish, Lis, Lev G, Schumacher, Robert J, Norris, Beverly J, Morgan, Monique L, Cuellar, Rebecca A. D, Blazar, Bruce R, Suryanarayanan, Raj, Gurvich, Vadim J, Georg, Gunda I

“…A disodium phosphonooxymethyl prodrug of the antitumor agent triptolide was prepared from the natural product in three steps (39% yield) and displayed…”
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Discovery of a Potential Allosteric Ligand Binding Site in CDK2 by Betzi, Stephane, Alam, Riazul, Martin, Mathew, Lubbers, Donna J, Han, Huijong, Jakkaraj, Sudhakar R, Georg, Gunda I, Schönbrunn, Ernst

“…Cyclin-dependent kinases (CDKs) are key regulatory enzymes in cell cycle progression and transcription. Aberrant activity of CDKs has been implicated in a…”
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Synthesis of Skeletally Diverse and Stereochemically Complex Library Templates Derived from Isosteviol and Steviol by Hutt, Oliver E, Doan, Trinh L, Georg, Gunda I

“…We have applied a diversity-oriented approach for the synthesis of skeletally diverse and stereochemically complex templates for small-molecule library…”
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Transition Metal-Free Direct Trifluoromethylation of 2,3-Dihydropyridin-4(1H)-ones at Room Temperature by Yu, Yi-Yun, Ranade, Adwait R., Georg, Gunda I.

“…A transition metal‐free, regioselective C‐5 trifluoromethylation of 2,3‐dihydropyridin‐4(1H)‐ones (cyclic enaminones) with trimethyl(trifluoromethyl)silane…”
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Development of Highly Potent and Selective Diaminothiazole Inhibitors of Cyclin-Dependent Kinases by Schonbrunn, Ernst, Betzi, Stephane, Alam, Riazul, Martin, Mathew P, Becker, Andreas, Han, Huijong, Francis, Rawle, Chakrasali, Ramappa, Jakkaraj, Sudhakar, Kazi, Aslamuzzaman, Sebti, Said M, Cubitt, Christopher L, Gebhard, Anthony W, Hazlehurst, Lori A, Tash, Joseph S, Georg, Gunda I

“…Cyclin-dependent kinases (CDKs) are serine/threonine protein kinases that act as key regulatory elements in cell cycle progression. We describe the development…”
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Synthesis of Strained 1,3-Diene Macrocycles via Copper-Mediated Castro–Stephens Coupling/Alkyne Reduction Tandem Reactions by Li, Wei, Schneider, Christopher M, Georg, Gunda I

“…A copper-mediated macrocyclization involving the reaction of a vinyl iodide and a terminal alkyne followed by an in situ reduction of the enyne intermediate is…”
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N -Butyldeoxygalactonojirimycin Induces Reversible Infertility in Male CD Rats by Gupta, Vijayalaxmi, Hild, Sheri A, Jakkaraj, Sudhakar R, Carlson, Erick J, Wong, Henry L, Allen, C. Leigh, Georg, Gunda I, Tash, Joseph S

“…This study shows for the first time that an iminosugar exerts anti-spermiogenic effect, inducing reversible infertility in a species that is not related to…”
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The Ecstasy and Agony of Assay Interference Compounds by Aldrich, Courtney, Bertozzi, Carolyn, Georg, Gunda I, Kiessling, Laura, Lindsley, Craig, Liotta, Dennis, Merz, Jr, Kenneth M, Schepartz, Alanna, Wang, Shaomeng

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Synthesis of 6- and 7-Membered Cyclic Enaminones: Scope and Mechanism by Niphakis, Micah J, Turunen, Brandon J, Georg, Gunda I

“…Six- and seven-membered cyclic enaminones can be prepared using common, environmentally benign reagents. Amino acids are used as synthetic precursors allowing…”
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