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Volume 58; Issue 6

Journal of Medicinal Chemistry

Volume 58; Issue 6

1

Targeting DNA Methylation with Small Molecules: What’s Next?

Erdmann, Alexandre, Halby, Ludovic, Fahy, Jacques, Arimondo, Paola B

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 1.75 MB

english, 2015

2

CNS Drug Design: Balancing Physicochemical Properties for Optimal Brain Exposure

Rankovic, Zoran

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 1.26 MB

english, 2015

3

Discovery of ( R )-1-(3-((2-Chloro-4-(((2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethyl)amino)methyl)-5-methoxyphenyl)amino)-3-oxopropyl)piperidin-4-yl [1,1′-Biphenyl]-2-ylcarbamate (TD-5959, GSK961081, Batefenterol): First-in-Class Dual Pharmacology Multivalent Muscarinic Antagonist and β 2 Agonist (MABA) for the Treatment of Chronic Obstructive Pulmonary Disease (COPD)

Hughes, Adam D., Chen, Yan, Hegde, Sharath S., Jasper, Jeffrey R., Jaw-Tsai, Sarah, Lee, Tae-Weon, McNamara, Alexander, Pulido-Rios, M. Teresa, Steinfeld, Tod, Mammen, Mathai

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 3.19 MB

english, 2015

4

Identification of Novel Aldose Reductase Inhibitors Based on Carboxymethylated Mercaptotriazinoindole Scaffold

Stefek, Milan, Soltesova Prnova, Marta, Majekova, Magdalena, Rechlin, Chris, Heine, Andreas, Klebe, Gerhard

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 3.21 MB

english, 2015

5

Discovery of a Series of Efficient, Centrally Efficacious BACE1 Inhibitors through Structure-Based Drug Design

Butler, Christopher R., Brodney, Michael A., Beck, Elizabeth M., Barreiro, Gabriela, Nolan, Charles E., Pan, Feng, Vajdos, Felix, Parris, Kevin, Varghese, Alison H., Helal, Christopher J., Lira, Ricar

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 3.06 MB

english, 2015

6

Structure-Based Evaluation of Non-nucleoside Inhibitors with Improved Potency and Solubility That Target HIV Reverse Transcriptase Variants

Frey, Kathleen M., Puleo, David E., Spasov, Krasimir A., Bollini, Mariella, Jorgensen, William L., Anderson, Karen S.

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 6.69 MB

english, 2015

7

Discovery of Imidazo[2,1- b ]thiazole HCV NS4B Inhibitors Exhibiting Synergistic Effect with Other Direct-Acting Antiviral Agents

Wang, Ning-Yu, Xu, Ying, Zuo, Wei-Qiong, Xiao, Kun-Jie, Liu, Li, Zeng, Xiu-Xiu, You, Xin-Yu, Zhang, Li-Dan, Gao, Chao, Liu, Zhi-Hao, Ye, Ting-Hong, Xia, Yong, Xiong, Ying, Song, Xue-Jiao, Lei, Qian, P

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 1.15 MB

english, 2015

8

Tailored Near-Infrared Contrast Agents for Image Guided Surgery

Njiojob, Costyl N., Owens, Eric A., Narayana, Lakshminarayana, Hyun, Hoon, Choi, Hak Soo, Henary, Maged

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 6.45 MB

english, 2015

9

The Discovery of Macrocyclic XIAP Antagonists from a DNA-Programmed Chemistry Library, and Their Optimization To Give Lead Compounds with in Vivo Antitumor Activity

Seigal, Benjamin A., Connors, William H., Fraley, Andrew, Borzilleri, Robert M., Carter, Percy H., Emanuel, Stuart L., Fargnoli, Joseph, Kim, Kyoung, Lei, Ming, Naglich, Joseph G., Pokross, Matthew E.

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 1.52 MB

english, 2015

10

Molecular Determinants of Biased Agonism at the Dopamine D 2 Receptor

Weichert, Dietmar, Banerjee, Ashutosh, Hiller, Christine, Kling, Ralf C., Hübner, Harald, Gmeiner, Peter

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 2.54 MB

english, 2015

11

Discovery and Optimization of a Novel Series of Dyrk1B Kinase Inhibitors To Explore a MEK Resistance Hypothesis

Kettle, Jason G., Ballard, Peter, Bardelle, Catherine, Cockerill, Mark, Colclough, Nicola, Critchlow, Susan E., Debreczeni, Judit, Fairley, Gary, Fillery, Shaun, Graham, Mark A., Goodwin, Louise, Guic

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 2.67 MB

english, 2015

12

2-Aryl-3-methyloctahydrophenanthrene-2,3,7-triols as Potent Dissociated Glucocorticoid Receptor Agonists

Chantigny, Yves A., Murray, John C., Kleinman, Edward F., Robinson, Ralph P., Plotkin, Michael A., Reese, Matthew R., Buckbinder, Leonard, McNiff, Patricia A., Millham, Michele L., Schaefer, Jean F.,

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 1.61 MB

english, 2015

13

A Novel Cell-Permeable, Selective, and Noncompetitive Inhibitor of KAT3 Histone Acetyltransferases from a Combined Molecular Pruning/Classical Isosterism Approach

Milite, Ciro, Feoli, Alessandra, Sasaki, Kazuki, La Pietra, Valeria, Balzano, Amodio Luca, Marinelli, Luciana, Mai, Antonello, Novellino, Ettore, Castellano, Sabrina, Tosco, Alessandra, Sbardella, Gia

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 4.44 MB

english, 2015

14

Development of Novel ACK1/TNK2 Inhibitors Using a Fragment-Based Approach

Lawrence, Harshani R., Mahajan, Kiran, Luo, Yunting, Zhang, Daniel, Tindall, Nathan, Huseyin, Miles, Gevariya, Harsukh, Kazi, Sakib, Ozcan, Sevil, Mahajan, Nupam P., Lawrence, Nicholas J.

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 2.92 MB

english, 2015

15

9 H -Purine Scaffold Reveals Induced-Fit Pocket Plasticity of the BRD9 Bromodomain

Picaud, Sarah, Strocchia, Maria, Terracciano, Stefania, Lauro, Gianluigi, Mendez, Jacqui, Daniels, Danette L., Riccio, Raffaele, Bifulco, Giuseppe, Bruno, Ines, Filippakopoulos, Panagis

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 892 KB

english, 2015

16

Design and Synthesis of Orally Bioavailable Aminopyrrolidinone Histone Deacetylase 6 Inhibitors

Lin, Xianfeng, Chen, Wenming, Qiu, Zongxing, Guo, Lei, Zhu, Wei, Li, Wentao, Wang, Zhanguo, Zhang, Weixing, Zhang, Zhenshan, Rong, Yiping, Zhang, Meifang, Yu, Lingjie, Zhong, Sheng, Zhao, Rong, Wu, Xi

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 630 KB

english, 2015

17

Discovery of Novel P1 Groups for Coagulation Factor VIIa Inhibition Using Fragment-Based Screening

Cheney, Daniel L., Bozarth, Jeffrey M., Metzler, William J., Morin, Paul E., Mueller, Luciano, Newitt, John A., Nirschl, Alexandra H., Rendina, Alan R., Tamura, James K., Wei, Anzhi, Wen, Xiao, Wurtz,

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 435 KB

english, 2015

18

Correction to “Design, Synthesis, and Structure–Activity Relationship of a Novel Series of GluN2C-Selective Potentiators”

Zimmerman, Sommer S., Khatri, Alpa, Garnier-Amblard, Ethel C., Mullasseril, Praseeda, Kurtkaya, Natalie L., Gyoneva, Stefka, Hansen, Kasper B., Traynelis, Stephen F., Liotta, Dennis C.

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 173 KB

english, 2015

19

Design, Synthesis, and Evaluation of NO-Donor Containing Carbonic Anhydrase Inhibitors To Lower Intraocular Pressure

Huang, Qinhua, Rui, Eugene Y., Cobbs, Morena, Dinh, Dac M., Gukasyan, Hovhannes J., Lafontaine, Jennifer A., Mehta, Saurabh, Patterson, Brian D., Rewolinski, David A., Richardson, Paul F., Edwards, Ma

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 2.44 MB

english, 2015

20

Design and Synthesis of Norendoxifen Analogues with Dual Aromatase Inhibitory and Estrogen Receptor Modulatory Activities

Lv, Wei, Liu, Jinzhong, Skaar, Todd C., Flockhart, David A., Cushman, Mark

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 3.27 MB

english, 2015