Search Results - "Evindar, Ghotas"

Parallel Synthesis of a Library of Benzoxazoles and Benzothiazoles Using Ligand-Accelerated Copper-Catalyzed Cyclizations of ortho-Halobenzanilides by Evindar, Ghotas, Batey, Robert A

“…A general method for the formation of benzoxazoles via a copper-catalyzed cyclization of ortho-haloanilides is reported. This approach complements the more…”
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Copper-Catalyzed Domino Annulation Approaches to the Synthesis of Benzoxazoles under Microwave-Accelerated and Conventional Thermal Conditions by Viirre, Russell D, Evindar, Ghotas, Batey, Robert A

“…Two domino annulation approaches for benzoxazole synthesis have been developed. In the first approach, copper-catalyzed intermolecular cross-coupling of…”
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Discovery of Thieno[3,2‑d]pyrimidine-6-carboxamides as Potent Inhibitors of SIRT1, SIRT2, and SIRT3 by Disch, Jeremy S, Evindar, Ghotas, Chiu, Cynthia H, Blum, Charles A, Dai, Han, Jin, Lei, Schuman, Eli, Lind, Kenneth E, Belyanskaya, Svetlana L, Deng, Jianghe, Coppo, Frank, Aquilani, Leah, Graybill, Todd L, Cuozzo, John W, Lavu, Siva, Mao, Cheney, Vlasuk, George P, Perni, Robert B

“…The sirtuins SIRT1, SIRT2, and SIRT3 are NAD+ dependent deacetylases that are considered potential targets for metabolic, inflammatory, oncologic, and…”
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Design and Application of a DNA-Encoded Macrocyclic Peptide Library by Zhu, Zhengrong, Shaginian, Alex, Grady, LaShadric C, O’Keeffe, Thomas, Shi, Xiangguo E, Davie, Christopher P, Simpson, Graham L, Messer, Jeffrey A, Evindar, Ghotas, Bream, Robert N, Thansandote, Praew P, Prentice, Naomi R, Mason, Andrew M, Pal, Sandeep

“…A DNA-encoded macrocyclic peptide library was designed and synthesized with 2.4 × 1012 members composed of 4–20 natural and non-natural amino acids…”
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Application of encoded library technology (ELT) to a protein–protein interaction target: Discovery of a potent class of integrin lymphocyte function-associated antigen 1 (LFA-1) antagonists by Kollmann, Christopher S., Bai, Xiaopeng, Tsai, Ching-Hsuan, Yang, Hongfang, Lind, Kenneth E., Skinner, Steven R., Zhu, Zhengrong, Israel, David I., Cuozzo, John W., Morgan, Barry A., Yuki, Koichi, Xie, Can, Springer, Timothy A., Shimaoka, Motomu, Evindar, Ghotas

“…Encoded library technology (ELT) was utilized to identify a class of compounds that disrupt the interaction between lymphocyte function-associated antigen-1…”
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Copper- and Palladium-Catalyzed Intramolecular Aryl Guanidinylation:  An Efficient Method for the Synthesis of 2-Aminobenzimidazoles by Evindar, Ghotas, Batey, Robert A

“…The formation of 2-aminobenzimidazoles via intramolecular C−N bond formation between an aryl halide and a guanidine moiety can be achieved using either copper…”
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Discovery and Characterization of a Class of Pyrazole Inhibitors of Bacterial Undecaprenyl Pyrophosphate Synthase by Concha, Nestor, Huang, Jianzhong, Bai, Xiaopeng, Benowitz, Andrew, Brady, Pat, Grady, LaShadric C, Kryn, Luz Helena, Holmes, David, Ingraham, Karen, Jin, Qi, Pothier Kaushansky, Laura, McCloskey, Lynn, Messer, Jeffrey A, O’Keefe, Heather, Patel, Amish, Satz, Alexander L, Sinnamon, Robert H, Schneck, Jessica, Skinner, Steve R, Summerfield, Jennifer, Taylor, Amy, Taylor, J. David, Evindar, Ghotas, Stavenger, Robert A

“…Undecaprenyl pyrophosphate synthase (UppS) is an essential enzyme in bacterial cell wall synthesis. Here we report the discovery of Staphylococcus aureus UppS…”
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Looking in the library by Johnson, Russell

“…Ghotas Evindar, Chemistry Group Leader at GlaxoSmithKline, talks with Nature Chemistry about the advantages of using encoded libraries in drug discovery and…”
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DNA-Encoded Library Technology-Based Discovery, Lead Optimization, and Prodrug Strategy toward Structurally Unique Indoleamine 2,3-Dioxygenase-1 (IDO1) Inhibitors by Kazmierski, Wieslaw M, Xia, Bing, Miller, John, De la Rosa, Martha, Favre, David, Dunham, Richard M, Washio, Yoshiaki, Zhu, Zhengrong, Wang, Feng, Mebrahtu, Makda, Deng, Hongfeng, Basilla, Jonathan, Wang, Liping, Evindar, Ghotas, Fan, Lijun, Olszewski, Alison, Prabhu, Ninad, Davie, Christopher, Messer, Jeffrey A, Samano, Vicente

“…We report the discovery of a novel indoleamine 2,3-dioxygenase-1 (IDO1) inhibitor class through the affinity selection of a previously unreported indole-based…”
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Synthesis of N-protected N-methyl serine and threonine by Luo, Yue, Evindar, Ghotas, Fishlock, Dan, Lajoie, Gilles A

“…Two efficient and convenient syntheses of N-Cbz and N-Fmoc N-methyl serine and threonine are described. The amino acid side-chain alcohol can be protected as a…”
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Encoded Library Technology as a Source of Hits for the Discovery and Lead Optimization of a Potent and Selective Class of Bactericidal Direct Inhibitors of Mycobacterium tuberculosis InhA by Encinas, Lourdes, O’Keefe, Heather, Neu, Margarete, Remuiñán, Modesto J, Patel, Amish M, Guardia, Ana, Davie, Christopher P, Pérez-Macías, Natalia, Yang, Hongfang, Convery, Maire A, Messer, Jeff A, Pérez-Herrán, Esther, Centrella, Paolo A, Álvarez-Gómez, Daniel, Clark, Matthew A, Huss, Sophie, O’Donovan, Gary K, Ortega-Muro, Fátima, McDowell, William, Castañeda, Pablo, Arico-Muendel, Christopher C, Pajk, Stane, Rullás, Joaquín, Angulo-Barturen, Iñigo, Álvarez-Ruíz, Emilio, Mendoza-Losana, Alfonso, Ballell Pages, Lluís, Castro-Pichel, Julia, Evindar, Ghotas

“…Tuberculosis (TB) is one of the world’s oldest and deadliest diseases, killing a person every 20 s. InhA, the enoyl-ACP reductase from Mycobacterium…”
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Prioritizing multiple therapeutic targets in parallel using automated DNA-encoded library screening by Machutta, Carl A., Kollmann, Christopher S., Lind, Kenneth E., Bai, Xiaopeng, Chan, Pan F., Huang, Jianzhong, Ballell, Lluis, Belyanskaya, Svetlana, Besra, Gurdyal S., Barros-Aguirre, David, Bates, Robert H., Centrella, Paolo A., Chang, Sandy S., Chai, Jing, Choudhry, Anthony E., Coffin, Aaron, Davie, Christopher P., Deng, Hongfeng, Deng, Jianghe, Ding, Yun, Dodson, Jason W., Fosbenner, David T., Gao, Enoch N., Graham, Taylor L., Graybill, Todd L., Ingraham, Karen, Johnson, Walter P., King, Bryan W., Kwiatkowski, Christopher R., Lelièvre, Joël, Li, Yue, Liu, Xiaorong, Lu, Quinn, Lehr, Ruth, Mendoza-Losana, Alfonso, Martin, John, McCloskey, Lynn, McCormick, Patti, O’Keefe, Heather P., O’Keeffe, Thomas, Pao, Christina, Phelps, Christopher B., Qi, Hongwei, Rafferty, Keith, Scavello, Genaro S., Steiginga, Matt S., Sundersingh, Flora S., Sweitzer, Sharon M., Szewczuk, Lawrence M., Taylor, Amy, Toh, May Fern, Wang, Juan, Wang, Minghui, Wilkins, Devan J., Xia, Bing, Yao, Gang, Zhang, Jean, Zhou, Jingye, Donahue, Christine P., Messer, Jeffrey A., Holmes, David, Arico-Muendel, Christopher C., Pope, Andrew J., Gross, Jeffrey W., Evindar, Ghotas

“…The identification and prioritization of chemically tractable therapeutic targets is a significant challenge in the discovery of new medicines. We have…”
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In Vivo Half-Life Extension of BMP1/TLL Metalloproteinase Inhibitors Using Small-Molecule Human Serum Albumin Binders by Vantourout, Julien C, Mason, Andrew M, Yuen, Josephine, Simpson, Graham L, Evindar, Ghotas, Kuai, Letian, Hobbs, Michael, Edgar, Emma, Needle, Saul, Bai, Xiaopeng, Wilson, Steve, Scott-Stevens, Paul, Traylen, William, Lambert, Kim, Young, Neil, Bunally, Shenaz, Summerfield, Scott G, Snell, Richard, Lad, Rakesh, Shi, Eric, Skinner, Steven, Shewchuk, Lisa, Watson, Allan J.B, Chung, Chun-wa, Pal, Sandeep, Holt, Dennis A, Kallander, Lara S, Prendergast, Joanne, Rivera, Katrina, Washburn, David G, Harpel, Mark R, Arico-Muendel, Christopher, Isidro-Llobet, Albert

“…Reducing the required frequence of drug dosing can improve the adherence of patients to chronic treatments. Hence, drugs with longer in vivo half-lives are…”
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Discovery of a Potent Class of PI3Kα Inhibitors with Unique Binding Mode via Encoded Library Technology (ELT) by Yang, Hongfang, Medeiros, Patricia F, Raha, Kaushik, Elkins, Patricia, Lind, Kenneth E, Lehr, Ruth, Adams, Nicholas D, Burgess, Joelle L, Schmidt, Stanley J, Knight, Steven D, Auger, Kurt R, Schaber, Michael D, Franklin, G. Joseph, Ding, Yun, DeLorey, Jennifer L, Centrella, Paolo A, Mataruse, Sibongile, Skinner, Steven R, Clark, Matthew A, Cuozzo, John W, Evindar, Ghotas

“…In the search of PI3K p110α wild type and H1047R mutant selective small molecule leads, an encoded library technology (ELT) campaign against the desired target…”
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Development of a Selection Method for Discovering Irreversible (Covalent) Binders from a DNA-Encoded Library by Zhu, Zhengrong, Grady, LaShadric C, Ding, Yun, Lind, Kenneth E, Davie, Christopher P, Phelps, Christopher B, Evindar, Ghotas

“…DNA-encoded libraries (DELs) have been broadly applied to identify chemical probes for target validation and lead discovery. To date, the main application of…”
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Correction: Author Correction: Prioritizing multiple therapeutic targets in parallel using automated DNA-encoded library screening by Machutta, Carl A., Kollmann, Christopher S., Lind, Kenneth E., Bai, Xiaopeng, Chan, Pan F., Huang, Jianzhong, Ballell, Lluis, Belyanskaya, Svetlana, Besra, Gurdyal S., Barros-Aguirre, David, Bates, Robert H., Centrella, Paolo A., Chang, Sandy S., Chai, Jing, Choudhry, Anthony E., Coffin, Aaron, Davie, Christopher P., Deng, Hongfeng, Deng, Jianghe, Ding, Yun, Dodson, Jason W., Fosbenner, David T., Gao, Enoch N., Graham, Taylor L., Graybill, Todd L., Ingraham, Karen, Johnson, Walter P., King, Bryan W., Kwiatkowski, Christopher R., Lelièvre, Joël, Li, Yue, Liu, Xiaorong, Lu, Quinn, Lehr, Ruth, Mendoza-Losana, Alfonso, Martin, John, McCloskey, Lynn, McCormick, Patti, O’Keefe, Heather P., O’Keeffe, Thomas, Pao, Christina, Phelps, Christopher B., Qi, Hongwei, Rafferty, Keith, Scavello, Genaro S., Steiginga, Matt S., Sundersingh, Flora S., Sweitzer, Sharon M., Szewczuk, Lawrence M., Taylor, Amy, Fern Toh, May, Wang, Juan, Wang, Minghui, Wilkins, Devan J., Xia, Bing, Yao, Gang, Zhang, Jean, Zhou, Jingye, Donahue, Christine P., Messer, Jeffrey A., Holmes, David, Arico-Muendel, Christopher C., Pope, Andrew J., Gross, Jeffrey W., Evindar, Ghotas

“…Nature Communications 8: Article number: 16081 (2017); Published: 17 July 2017, Updated: 13 July 2018 The original version of this Article omitted the…”
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Discovery of Clinical Candidate GSK1842799 As a Selective S1P1 Receptor Agonist (Prodrug) for Multiple Sclerosis by Deng, Hongfeng, Bernier, Sylvie G, Doyle, Elisabeth, Lorusso, Jeanine, Morgan, Barry A, Westlin, William F, Evindar, Ghotas

“…To develop effective oral treatment for multiple sclerosis (MS), we discovered a series of alkyl-substituted biaryl amino alcohols as selective S1P1…”
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The Discovery of VX-745: A Novel and Selective p38α Kinase Inhibitor by Duffy, John P, Harrington, Edmund M, Salituro, Francesco G, Cochran, John E, Green, Jeremy, Gao, Huai, Bemis, Guy W, Evindar, Ghotas, Galullo, Vincent P, Ford, Pamella J, Germann, Ursula A, Wilson, Keith P, Bellon, Steven F, Chen, Guanging, Taslimi, Paul, Jones, Peter, Huang, Cassey, Pazhanisamy, S, Wang, Yow-Ming, Murcko, Mark A, Su, Michael S.S

“…The synthesis of novel, selective, orally active 2,5-disubstituted 6H-pyrimido[1,6-b]pyridazin-6-one p38α inhibitors is described. Application of structural…”
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Exploring amino acids derivatives as potent, selective, and direct agonists of sphingosine-1-phosphate receptor subtype-1 by Evindar, Ghotas, Deng, Hongfeng, Bernier, Sylvie G, Doyle, Elisabeth, Lorusso, Jeanine, Morgan, Barry A, Westlin, William F

“…In the quest to discover a potent and selective class of direct agonists to the sphingosine-1-phosphate receptor, we explored the carboxylate functional group…”
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Discovery of Clinical Candidate GSK1842799 As a Selective S1P 1 Receptor Agonist (Prodrug) for Multiple Sclerosis by Deng, Hongfeng, Bernier, Sylvie G., Doyle, Elisabeth, Lorusso, Jeanine, Morgan, Barry A., Westlin, William F., Evindar, Ghotas

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