Orchestrated Triple CH Activation Reactions Using Two Directing Groups: Rapid Assembly of Complex Pyrazoles von Yang, Weibo, Ye, Shengqing, Fanning, Dewey, Coon, Timothy, Schmidt, Yvonne, Krenitsky, Paul, Stamos, Dean, Yu, Jin-Quan

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Novel Dual-Targeting Benzimidazole Urea Inhibitors of DNA Gyrase and Topoisomerase IV Possessing Potent Antibacterial Activity: Intelligent Design and Evolution through the Judicio... von Charifson, Paul S, Grillot, Anne-Laure, Grossman, Trudy H, Parsons, Jonathan D, Badia, Michael, Bellon, Steve, Deininger, David D, Drumm, Joseph E, Gross, Christian H, LeTiran, Arnaud, Liao, Yusheng, Mani, Nagraj, Nicolau, David P, Perola, Emanuele, Ronkin, Steven, Shannon, Dean, Swenson, Lora L, Tang, Qing, Tessier, Pamela R, Tian, Ski-Kai, Trudeau, Martin, Wang, Tiansheng, Wei, Yunyi, Zhang, Hong, Stamos, Dean

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A novel CCR2 antagonist inhibits atherogenesis in apoE deficient mice by achieving high receptor occupancy von Bot, Ilze, Ortiz Zacarías, Natalia V., de Witte, Wilhelmus E. A., de Vries, Henk, van Santbrink, Peter J., van der Velden, Daniël, Kröner, Mara J., van der Berg, Dirk-Jan, Stamos, Dean, de Lange, Elizabeth C. M., Kuiper, Johan, IJzerman, Adriaan P., Heitman, Laura H.

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Discovery of pyrazolthiazoles as novel and potent inhibitors of bacterial gyrase von Ronkin, Steven M., Badia, Michael, Bellon, Steve, Grillot, Anne-Laure, Gross, Christian H., Grossman, Trudy H., Mani, Nagraj, Parsons, Jonathan D., Stamos, Dean, Trudeau, Martin, Wei, Yunyi, Charifson, Paul S.

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When structure–affinity relationships meet structure–kinetics relationships: 3-((Inden-1-yl)amino)-1-isopropyl-cyclopentane-1-carboxamides as CCR2 antagonists von Vilums, Maris, Zweemer, Annelien J.M., Barmare, Farhana, van der Gracht, Anouk M.F., Bleeker, Dave C.T., Yu, Zhiyi, de Vries, Henk, Gross, Raymond, Clemens, Jeremy, Krenitsky, Paul, Brussee, Johannes, Stamos, Dean, Saunders, John, Heitman, Laura H., IJzerman, Adriaan P.

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Dual Targeting of GyrB and ParE by a Novel Aminobenzimidazole Class of Antibacterial Compounds von GROSSMAN, Trudy H, BARTELS, Douglas J, MANI, Nagraj, MULLIN, Steve, GROSS, Christian H, PARSONS, Jonathan D, YUSHENG LIAO, GRILLOT, Anne-Laure, STAMOS, Dean, OLSON, Eric R, CHARIFSON, Paul S

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In Vitro Characterization of the Antibacterial Spectrum of Novel Bacterial Type II Topoisomerase Inhibitors of the Aminobenzimidazole Class von MANI, Nagraj, GROSS, Christian H, GROSSMAN, Trudy H, PARSONS, Jonathan D, HANZELKA, Brian, MÜH, Ute, MULLIN, Steve, YUSHENG LIAO, GRILLOT, Anne-Laure, STAMOS, Dean, CHARIFSON, Paul S

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Evaluation of (4-Arylpiperidin-1-yl)cyclopentanecarboxamides As High-Affinity and Long-Residence-Time Antagonists for the CCR2 Receptor von Vilums, Maris, Zweemer, Annelien J. M., Dilanchian, Arian, van Veldhoven, Jacobus P. D., de Vries, Henk, Brussee, Johannes, Saunders, John, Stamos, Dean, Heitman, Laura H., IJzerman, Adriaan P.

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A mild preparation of vinyliodides from vinylsilanes von Stamos, Dean P, Taylor, Andrew G, Kishi, Yoshito

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Ligand-Promoted C(sp3)−H Olefination en Route to Multi-functionalized Pyrazoles von Yang, Weibo, Ye, Shengqing, Schmidt, Yvonne, Stamos, Dean, Yu, Jin-Quan

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Synthetic studies on halichondrins: A practical synthesis of the C.1C.13 segment von Stamos, Dean P, Kishi, Yoshito

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New Synthetic Route to the C.14−C.38 Segment of Halichondrins von Stamos, Dean P, Chen, Sean S, Kishi, Yoshito

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Abstract 6411: Discovery of covalent ligands to novel E3 ligases enables bispecific degraders with highly differentiated protein degradation across a broad range of targets von Baltgalvis, Kristen, Kikuchi, Shota, Symons, Kent, Klebba, Joseph, Luukkonen, Lena, Naro, Yuta, Walsh, Colin, Chang, Joon, Chapman, Charles, Tabatabaei, Ali, Nordin, Brian, Eissler, Christie, Chick, Joel, Whitby, Landon, Brannon, Jaclyn, Simon, Gabe, Patricelli, Matt, Stamos, Dean, Burgess, Larry, Kinsella, Todd

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Identification of Novel HSP90α/β Isoform Selective Inhibitors Using Structure-Based Drug Design. Demonstration of Potential Utility in Treating CNS Disorders such as Huntington’s D... von Ernst, Justin T, Neubert, Timothy, Liu, Michael, Sperry, Samuel, Zuccola, Harmon, Turnbull, Amy, Fleck, Beth, Kargo, William, Woody, Lisa, Chiang, Peggy, Tran, Dao, Chen, Weichao, Snyder, Phillip, Alcacio, Timothy, Nezami, Azin, Reynolds, James, Alvi, Khisal, Goulet, Lance, Stamos, Dean

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NHC-Pd(II) Catalyzed Methylene C(sp3)–H Arylation of Piperidines and Tetrahydropyrans von Ye, Shengqing, Yang, Weibo, Coon, Timothy, Fanning, Dewey, Neubert, Tim, Stamos, Dean, Yu, Jin-Quan

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Structure–Kinetic RelationshipsAn Overlooked Parameter in Hit-to-Lead Optimization: A Case of Cyclopentylamines as Chemokine Receptor 2 Antagonists von Vilums, Maris, Zweemer, Annelien J. M, Yu, Zhiyi, de Vries, Henk, Hillger, Julia M, Wapenaar, Hannah, Bollen, Ilse A. E, Barmare, Farhana, Gross, Raymond, Clemens, Jeremy, Krenitsky, Paul, Brussee, Johannes, Stamos, Dean, Saunders, John, Heitman, Laura H, IJzerman, Adriaan P

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Orchestrated Triple CH Activation Reactions Using Two Directing Groups: Rapid Assembly of Complex Pyrazoles von Yang, Weibo, Ye, Shengqing, Fanning, Dewey, Coon, Timothy, Schmidt, Yvonne, Krenitsky, Paul, Stamos, Dean, Yu, Jin-Quan

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Abstract 11581: Longer Receptor Residence Times Improve the Effectiveness of CCR2 Antagonists in the Prevention of Atherosclerosis von Bot, Ilze, Ortiz Zacarias, Natalia V, de Vries, Henk, van Santbrink, Peter J, van der Velden, Daniel, Kuiper, Johan, Stamos, Dean, IJzerman, Adriaan P, Heitman, Laura H

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Correlation between chemotype-dependent binding conformations of HSP90I-/I2 and isoform selectivityaImplications for the structure-based design of HSP90I-/I2 selective inhibitors f... von Ernst, Justin, Liu, Michael, Zuccola, Harmon, Neubert, Timothy, Beaumont, Kevin, Turnbull, Amy, Kallel, Adam, Vought, Bryan, Stamos, Dean

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Successful application of serum shift prediction models to the design of dual targeting inhibitors of bacterial gyrase B and topoisomerase IV with improved in vivo efficacy von Perola, Emanuele, Stamos, Dean, Grillot, Anne-Laure, Ronkin, Steven, Wang, Tiansheng, LeTiran, Arnaud, Tang, Qing, Deininger, David D., Liao, Yusheng, Tian, Shi-Kai, Drumm, Joseph E., Nicolau, David P., Tessier, Pamela R., Mani, Nagraj, Grossman, Trudy H., Charifson, Paul S.

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