Search Results - "Dhar, T G"

Organocatalyzed, Visible-Light Photoredox-Mediated, One-Pot Minisci Reaction Using Carboxylic Acids via N‑(Acyloxy)phthalimides by Sherwood, Trevor C, Li, Ning, Yazdani, Aliza N, Dhar, T. G. Murali

“…An improved, one-pot Minisci reaction has been developed using visible light, an organic photocatalyst, and carboxylic acids as radical precursors via the…”
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Ligand-Promoted Borylation of C(sp3)H Bonds with Palladium(II) Catalysts by He, Jian, Jiang, Heng, Takise, Ryosuke, Zhu, Ru-Yi, Chen, Gang, Dai, Hui-Xiong, Dhar, T. G. Murali, Shi, Jun, Zhang, Hao, Cheng, Peter T. W., Yu, Jin-Quan

“…A quinoline‐based ligand effectively promotes the palladium‐catalyzed borylation of C(sp3)H bonds. Primary β‐C(sp3)H bonds in carboxylic acid derivatives as…”
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Complex molecule synthesis by electrocatalytic decarboxylative cross-coupling by Zhang, Benxiang, He, Jiayan, Gao, Yang, Levy, Laura, Oderinde, Martins S., Palkowitz, Maximilian D., Dhar, T. G. Murali, Mandler, Michael D., Collins, Michael R., Schmitt, Daniel C., Bolduc, Philippe N., Chen, TeYu, Clementson, Sebastian, Petersen, Nadia Nasser, Laudadio, Gabriele, Bi, Cheng, Kawamata, Yu, Baran, Phil S.

“…Modern retrosynthetic analysis in organic chemistry is based on the principle of polar relationships between functional groups to guide the design of synthetic…”
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Synthesis of Cyclobutane-Fused Tetracyclic Scaffolds via Visible-Light Photocatalysis for Building Molecular Complexity by Oderinde, Martins S, Mao, Edna, Ramirez, Antonio, Pawluczyk, Joseph, Jorge, Christine, Cornelius, Lyndon A. M, Kempson, James, Vetrichelvan, Muthalagu, Pitchai, Manivel, Gupta, Anuradha, Gupta, Arun Kumar, Meanwell, Nicholas A, Mathur, Arvind, Dhar, T. G. Murali

“…We describe the synthesis through visible-light photocatalysis of novel functionalized tetracyclic scaffolds that incorporate a fused…”
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Synthesis of 1‑(tert-Butyl) 4‑Methyl (1R,2S,4R)‑2-Methylcyclohexane-1,4-dicarboxylate from Hagemann’s tert-Butyl Ester for an Improved Synthesis of BMS-986251 by Cornelius, Lyndon A. M, Li, Jianqing, Smith, Daniel, Krishnananthan, Subramaniam, Yip, Shiuhang, Wu, Dauh-Rurng, Pawluczyk, Joseph, Aulakh, Darpandeep, Sarjeant, Amy A, Kempson, James, Tino, Joseph A, Mathur, Arvind, Murali Dhar, T. G, Cherney, Robert J

“…We describe an efficient synthetic route to differentially protected diester, 1-(tert-butyl) 4-methyl (1R,2S,4R)-2-methylcyclohexane-1,4-dicarboxylate (+)-1,…”
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Intramolecular [2+2] Cycloaddition of N‐Allylcinnamamines and N‐Allylcinnamamides by Visible‐Light Photocatalysis by Oderinde, Martins S., Kempson, James, Smith, Daniel, Meanwell, Nicholas A., Mao, Edna, Pawluczyk, Joseph, Vetrichelvan, Muthalagu, Pitchai, Manivel, Karmakar, Ananta, Rampulla, Richard, Li, Jianqing, Murali Dhar, T. G., Mathur, Arvind

“…The visible light‐promoted intramolecular [2+2] cycloaddition of N‐allylcinnamamines and N‐allylcinnamamides in the presence of catalytic amounts of…”
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Photocatalytic Dearomative Intermolecular [2 + 2] Cycloaddition of Heterocycles for Building Molecular Complexity by Oderinde, Martins S, Ramirez, Antonio, Dhar, T G Murali, Cornelius, Lyndon A M, Jorge, Christine, Aulakh, Darpandeep, Sandhu, Bhupinder, Pawluczyk, Joseph, Sarjeant, Amy A, Meanwell, Nicholas A, Mathur, Arvind, Kempson, James

“…Indole and indoline rings are important pharmacophoric scaffolds found in marketed drugs, agrochemicals, and biologically active molecules. The [2 + 2]…”
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Identification of potent, selective and orally bioavailable phenyl ((R)-3-phenylpyrrolidin-3-yl)sulfone analogues as RORγt inverse agonists by Lu, Zhonghui, Duan, James J.-W., Xiao, Haiyun, Neels, James, Wu, Dauh-Rurng, Weigelt, Carolyn A., Sack, John S., Khan, Javed, Ruzanov, Max, An, Yongmi, Yarde, Melissa, Karmakar, Ananta, Vishwakrishnan, Sureshbabu, Baratam, Venkata, Shankarappa, Harisha, Vanteru, Sridhar, Babu, Venkatesh, Basha, Mushkin, Kumar Gupta, Arun, Kumaravel, Selvakumar, Mathur, Arvind, Zhao, Qihong, Salter-Cid, Luisa M., Carter, Percy H., Murali Dhar, T.G.

“…[Display omitted] An X-ray crystal structure of one of our previously discovered RORγt inverse agonists bound to the RORγt ligand binding domain revealed that…”
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Identification and Preclinical Pharmacology of ((1R,3S)‑1-Amino-3-((S)‑6-(2-methoxyphenethyl)-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986166): A Differentiated Sphingosine-1-phosphate Receptor 1 (S1P1) Modulator Advanced into Clinical Trials by Gilmore, John L, Xiao, Hai-Yun, Dhar, T. G. Murali, Yang, Michael G, Xiao, Zili, Xie, Jenny, Lehman-McKeeman, Lois D, Gong, Lei, Sun, Huadong, Lecureux, Lloyd, Chen, Cliff, Wu, Dauh-Rurng, Dabros, Marta, Yang, Xiaoxia, Taylor, Tracy L, Zhou, Xia D, Heimrich, Elizabeth M, Thomas, Rochelle, McIntyre, Kim W, Borowski, Virna, Warrack, Bethanne M, Li, Yuwen, Shi, Hong, Levesque, Paul C, Yang, Zheng, Marino, Anthony M, Cornelius, Georgia, D’Arienzo, Celia J, Mathur, Arvind, Rampulla, Richard, Gupta, Anuradha, Pragalathan, Bala, Shen, Ding Ren, Cvijic, Mary Ellen, Salter-Cid, Luisa M, Carter, Percy H, Dyckman, Alaric J

“…Recently, our research group reported the identification of BMS-986104 (2) as a differentiated S1P1 receptor modulator. In comparison to fingolimod (1), a full…”
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Discovery of 2,6–difluorobenzyl ether series of phenyl ((R)–3–phenylpyrrolidin–3–yl)sulfones as surprisingly potent, selective and orally bioavailable RORγt inverse agonists by Duan, James J.-W., Jiang, Bin, Lu, Zhonghui, Stachura, Sylwia, Weigelt, Carolyn A., Sack, John S., Khan, Javed, Ruzanov, Max, Wu, Dauh–Rurng, Yarde, Melissa, Shen, Ding–Ren, Zhao, Qihong, Salter–Cid, Luisa M., Carter, Percy H., Murali Dhar, T.G.

“…[Display omitted] In an effort to discover oral inverse agonists of RORγt to treat inflammatory diseases, a new 2,6–difluorobenzyl ether series of cyclopentyl…”
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Small Molecule Antagonist of Leukocyte Function Associated Antigen-1 (LFA-1): Structure−Activity Relationships Leading to the Identification of 6-((5S,9R)-9-(4-Cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]nonan-7-yl)nicotinic Acid (BMS-688521) by Watterson, Scott H, Xiao, Zili, Dodd, Dharmpal S, Tortolani, David R, Vaccaro, Wayne, Potin, Dominique, Launay, Michele, Stetsko, Dawn K, Skala, Stacey, Davis, Patric M, Lee, Deborah, Yang, Xiaoxia, McIntyre, Kim W, Balimane, Praveen, Patel, Karishma, Yang, Zheng, Marathe, Punit, Kadiyala, Pathanjali, Tebben, Andrew J, Sheriff, Steven, Chang, ChiehYing Y, Ziemba, Theresa, Zhang, Huiping, Chen, Bang-Chi, DelMonte, Albert J, Aranibar, Nelly, McKinnon, Murray, Barrish, Joel C, Suchard, Suzanne J, Murali Dhar, T. G

“…Leukocyte function-associated antigen-1 (LFA-1), also known as CD11a/CD18 or αLβ2, belongs to the β2 integrin subfamily and is constitutively expressed on all…”
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Identification of Tricyclic Agonists of Sphingosine-1-phosphate Receptor 1 (S1P1) Employing Ligand-Based Drug Design by Xiao, Hai-Yun, Watterson, Scott H, Langevine, Charles M, Srivastava, Anurag S, Ko, Soo S, Zhang, Yanlei, Cherney, Robert J, Guo, Wei-Wei, Gilmore, John L, Sheppeck, James E, Wu, Dauh-Rurng, Li, Peng, Ramasamy, Duraisamy, Arunachalam, Piramanayagam, Mathur, Arvind, Taylor, Tracy L, Shuster, David J, McIntyre, Kim W, Shen, Ding-Ren, Yarde, Melissa, Cvijic, Mary Ellen, Marino, Anthony M, Balimane, Praveen V, Yang, Zheng, Banas, Dana M, Cornelius, Georgia, D’Arienzo, Celia J, Warrack, Bethanne M, Lehman-McKeeman, Lois, Salter-Cid, Luisa M, Xie, Jenny, Barrish, Joel C, Carter, Percy H, Dyckman, Alaric J, Dhar, T. G. Murali

“…Fingolimod (1) is the first approved oral therapy for the treatment of relapsing remitting multiple sclerosis. While the phosphorylated metabolite of…”
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Novel Synthesis of the Hexahydroimidazo[1,5b]isoquinoline Scaffold: Application to the Synthesis of Glucocorticoid Receptor Modulators by Xiao, Hai-Yun, Wu, Dauh-Rurng, Malley, Mary F, Gougoutas, Jack Z, Habte, Sium F, Cunningham, Mark D, Somerville, John E, Dodd, John H, Barrish, Joel C, Nadler, Steven G, Dhar, T. G. Murali

“…The first stereoselective synthesis of the hexahydroimidazo[1,5b]isoquinoline (HHII) scaffold as a surrogate for the steroidal A-B ring system is described…”
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Perspectives on Nuclear Magnetic Resonance Spectroscopy in Drug Discovery Research by Caceres-Cortes, Janet, Falk, Bradley, Mueller, Luciano, Dhar, T G Murali

“…The drug discovery landscape has undergone a significant transformation over the past decade, owing to research endeavors in a wide range of areas leading to…”
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The identification of novel p38α isoform selective kinase inhibitors having an unprecedented p38α binding mode by Wrobleski, Stephen T., Lin, Shuqun, Murali Dhar, T.G., Dyckman, Alaric J., Li, Tianle, Pitt, Sidney, Zhang, Rosemary, Fan, Yi, Doweyko, Arthur M., Tokarski, John S., Kish, Kevin F., Kiefer, Susan E., Sack, John S., Newitt, John A., Witmer, Mark R., McKinnon, Murray, Barrish, Joel C., Dodd, John H., Schieven, Gary L., Leftheris, Katerina

“…A novel series of p38 MAP kinase inhibitors with high selectivity for the p38α isoform over the other family members including the highly homologous p38β…”
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Overcoming Limitations in Decarboxylative Arylation via Ag–Ni Electrocatalysis by Palkowitz, Maximilian D., Laudadio, Gabriele, Kolb, Simon, Choi, Jin, Oderinde, Martins S., Ewing, Tamara El-Hayek, Bolduc, Philippe N., Chen, TeYu, Zhang, Hao, Cheng, Peter T. W., Zhang, Benxiang, Mandler, Michael D., Blasczak, Vanna D., Richter, Jeremy M., Collins, Michael R., Schioldager, Ryan L., Bravo, Martin, Dhar, T. G. Murali, Vokits, Benjamin, Zhu, Yeheng, Echeverria, Pierre-Georges, Poss, Michael A., Shaw, Scott A., Clementson, Sebastian, Petersen, Nadia Nasser, Mykhailiuk, Pavel K., Baran, Phil S.

“…A useful protocol for achieving decarboxylative cross-coupling (DCC) of redox-active esters (RAE, isolated or generated in situ) and halo­(hetero)­arenes is…”
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Decarboxylative Intramolecular Arene Alkylation Using N‑(Acyloxy)phthalimides, an Organic Photocatalyst, and Visible Light by Sherwood, Trevor C, Xiao, Hai-Yun, Bhaskar, Roshan G, Simmons, Eric M, Zaretsky, Serge, Rauch, Martin P, Knowles, Robert R, Dhar, T. G. Murali

“…An intramolecular arene alkylation reaction has been developed using the organic photocatalyst 4CzIPN, visible light, and N-(acyloxy)­phthalimides as radical…”
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Antroquinonol A: Scalable Synthesis and Preclinical Biology of a Phase 2 Drug Candidate by Villaume, Matthew T, Sella, Eran, Saul, Garrett, Borzilleri, Robert M, Fargnoli, Joseph, Johnston, Kathy A, Zhang, Haiying, Fereshteh, Mark P, Dhar, T. G. Murali, Baran, Phil S

“…The fungal-derived Taiwanese natural product antroquinonol A has attracted both academic and commercial interest due to its reported exciting biological…”
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Urea based CCR3 antagonists employing a tetrahydro-1,3-oxazin-2-one spacer by Dhar, T.G. Murali, Yang, Guchen, Davies, Paul, Malley, Mary F., Gougoutas, Jack Z., Wu, Dauh-Rurng, Barrish, Joel C., Carter, Percy H.

“…Conformational restriction of open chain analogs with a more polar tetrahydro-1,3-oxazin-2-one spacer led to the identification of potent urea-based CCR3…”
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Discovery and Synthesis of Heterobifunctional Degraders of Rearranged during Transfection (RET) Kinase by Qiao, Jennifer X., Williams, David, Gill, Patrice, Li, Ling, Norris, Derek, Tokarski, John S., Wong, Jessica, Qi, Huilin, Hafeji, Yamnah, Downes, Daniel P., Degnen, Bill, Wang, Ying-Kai, Locke, Gregory, Fang, Hua, Yu, Fei, Xu, Songmei, Naglich, Joseph, Zhang, Jun, Nanjappa, Purushothama, Dai, Chao, Chourb, Lisa, Napoline, Jonathan, Tester, Richland, Jorge, Christine, Li, Yi-Xin, Mathur, Arvind, Barbieri, Christopher, Soars, Matthew G., Venkatanarayan, Avinashnarayan, Lees, Emma, Borzilleri, Robert M., Gavai, Ashvinikumar V., Wichroski, Michael, Dhar, T. G. Murali

“…We describe the design, synthesis, and structure–activity relationship (SAR) of heterobifunctional RET ligand-directed degraders (LDDs) derived from three…”
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