Volume 58; Issue 5

Journal of Medicinal Chemistry

Volume 58; Issue 5

1

Targeting Aldose Reductase for the Treatment of Diabetes Complications and Inflammatory Diseases: New Insights and Future Directions

Maccari, Rosanna, Ottanà, Rosaria

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 1.07 MB

english, 2015

2

Parallel Worlds of Public and Commercial Bioactive Chemistry Data

Lipinski, Christopher A., Litterman, Nadia K., Southan, Christopher, Williams, Antony J., Clark, Alex M., Ekins, Sean

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 921 KB

english, 2015

3

Selective Nonpeptidic Fluorescent Ligands for Oxytocin Receptor: Design, Synthesis, and Application to Time-Resolved FRET Binding Assay

Karpenko, Iuliia A., Margathe, Jean-François, Rodriguez, Thiéric, Pflimlin, Elsa, Dupuis, Elodie, Hibert, Marcel, Durroux, Thierry, Bonnet, Dominique

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 1020 KB

english, 2015

4

Synthesis and Structure–Activity Relationship Study of a New Series of Selective σ 1 Receptor Ligands for the Treatment of Pain: 4-Aminotriazoles

Díaz, José Luis, Christmann, Ute, Fernández, Ariadna, Torrens, Antoni, Port, Adriana, Pascual, Rosalia, Álvarez, Inés, Burgueño, Javier, Monroy, Xavier, Montero, Ana, Balada, Ariadna, Vela, José Migue

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 923 KB

english, 2015

5

Discovery of Highly Selective Brain-Penetrant Vasopressin 1a Antagonists for the Potential Treatment of Autism via a Chemogenomic and Scaffold Hopping Approach

Ratni, Hasane, Rogers-Evans, Mark, Bissantz, Caterina, Grundschober, Christophe, Moreau, Jean-Luc, Schuler, Franz, Fischer, Holger, Alvarez Sanchez, Ruben, Schnider, Patrick

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 923 KB

english, 2015

6

Engineering Potent and Selective Analogues of GpTx-1, a Tarantula Venom Peptide Antagonist of the Na V 1.7 Sodium Channel

Murray, Justin K., Ligutti, Joseph, Liu, Dong, Zou, Anruo, Poppe, Leszek, Li, Hongyan, Andrews, Kristin L., Moyer, Bryan D., McDonough, Stefan I., Favreau, Philippe, Stöcklin, Reto, Miranda, Les P.

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 2.68 MB

english, 2015

7

Discovery and Development of Galeterone (TOK-001 or VN/124-1) for the Treatment of All Stages of Prostate Cancer

Njar, Vincent C. O., Brodie, Angela M. H.

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 2.42 MB

english, 2015

8

FimH Antagonists: Bioisosteres To Improve the in Vitro and in Vivo PK/PD Profile

Kleeb, Simon, Pang, Lijuan, Mayer, Katharina, Eris, Deniz, Sigl, Anja, Preston, Roland C., Zihlmann, Pascal, Sharpe, Timothy, Jakob, Roman P., Abgottspon, Daniela, Hutter, Aline S., Scharenberg, Meike

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 3.15 MB

english, 2015

9

Discovery of Efficacious Pseudomonas aeruginosa -Targeted Siderophore-Conjugated Monocarbams by Application of a Semi-mechanistic Pharmacokinetic/Pharmacodynamic Model

Murphy-Benenato, Kerry E., Bhagunde, Pratik R., Chen, April, Davis, Hajnalka E., Durand-Réville, Thomas F., Ehmann, David E., Galullo, Vincent, Harris, Jennifer J., Hatoum-Mokdad, Holia, Jahić, Haris,

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 1.06 MB

english, 2015

10

Activity of 2-Aryl-2-(3-indolyl)acetohydroxamates against Drug-Resistant Cancer Cells

Aksenov, Alexander V., Smirnov, Alexander N., Magedov, Igor V., Reisenauer, Mary R., Aksenov, Nicolai A., Aksenova, Inna V., Pendleton, Alexander L., Nguyen, Gina, Johnston, Robert K., Rubin, Michael,

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 2.12 MB

english, 2015

11

Discovery of Novel 2,5-Dioxoimidazolidine-Based P2X 7 Receptor Antagonists as Constrained Analogues of KN62

Park, Jin-Hee, Lee, Ga-Eun, Lee, So-Deok, Hien, Tran Thi, Kim, Sujin, Yang, Jin Won, Cho, Joong-Heui, Ko, Hyojin, Lim, Sung-Chul, Kim, Yoon-Gyoon, Kang, Keon-Wook, Kim, Yong-Chul

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 1.17 MB

english, 2015

12

Stem Cell Mobilizers Targeting Chemokine Receptor CXCR4: Renoprotective Application in Acute Kidney Injury

Wu, Chien-Huang, Song, Jen-Shin, Chang, Kuei-Hua, Jan, Jiing-Jyh, Chen, Chiung-Tong, Chou, Ming-Chen, Yeh, Kai-Chia, Wong, Ying-Chieh, Tseng, Chen-Tso, Wu, Szu-Huei, Yeh, Ching-Fang, Huang, Chung-Yu,

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 1.36 MB

english, 2015

13

Selective, Nontoxic CB 2 Cannabinoid o -Quinone with in Vivo Activity against Triple-Negative Breast Cancer

Morales, Paula, Blasco-Benito, Sandra, Andradas, Clara, Gómez-Cañas, María, Flores, Juana María, Goya, Pilar, Fernández-Ruiz, Javier, Sánchez, Cristina, Jagerovic, Nadine

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 1.39 MB

english, 2015

14

Exploitation of the Ability of γ-Tocopherol to Facilitate Membrane Co-localization of Akt and PHLPP1 to Develop PHLPP1-Targeted Akt Inhibitors

Yan, Ribai, Chuang, Hsiao-Ching, Kapuriya, Naval, Chou, Chih-Chien, Lai, Po-Ting, Chang, Hsin-Wen, Yang, Chia-Ning, Kulp, Samuel K., Chen, Ching-Shih

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 9.43 MB

english, 2015

15

Understanding Our Love Affair with p -Chlorophenyl: Present Day Implications from Historical Biases of Reagent Selection

Brown, Dean G., Gagnon, Moriah M., Boström, Jonas

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 2.98 MB

english, 2015

16

Design, Synthesis, and Biological Evaluation of Theranostic Vitamin–Linker–Taxoid Conjugates

Vineberg, Jacob G., Wang, Tao, Zuniga, Edison S., Ojima, Iwao

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 2.23 MB

english, 2015

17

Strong Antibacterial Properties of Anion Transporters: A Result of Depolarization and Weakening of the Bacterial Membrane

Elie, Claude R., David, Guillaume, Schmitzer, Andreea R.

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 1.69 MB

english, 2015

18

C-Terminal Modifications of Apelin-13 Significantly Change Ligand Binding, Receptor Signaling, and Hypotensive Action

Murza, Alexandre, Besserer-Offroy, Élie, Côté, Jérôme, Bérubé, Patrick, Longpré, Jean-Michel, Dumaine, Robert, Lesur, Olivier, Auger-Messier, Mannix, Leduc, Richard, Sarret, Philippe, Marsault, Éric

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 767 KB

english, 2015

19

Structure-Guided Design of a Series of MCL-1 Inhibitors with High Affinity and Selectivity

Bruncko, Milan, Wang, Le, Sheppard, George S., Phillips, Darren C., Tahir, Stephen K., Xue, John, Erickson, Scott, Fidanze, Steve, Fry, Elizabeth, Hasvold, Lisa, Jenkins, Gary J., Jin, Sha, Judge, Rus

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 1.31 MB

english, 2015

20

Design and Optimization of a Series of 1-Sulfonylpyrazolo[4,3- b ]pyridines as Selective c-Met Inhibitors

Ma, Yuchi, Sun, Guangqiang, Chen, Danqi, Peng, Xia, Chen, Yue-Lei, Su, Yi, Ji, Yinchun, Liang, Jin, Wang, Xin, Chen, Lin, Ding, Jian, Xiong, Bing, Ai, Jing, Geng, Meiyu, Shen, Jingkang

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 1.74 MB

english, 2015

21

Structure-Based Lead Optimization and Biological Evaluation of BAX Direct Activators as Novel Potential Anticancer Agents

Stornaiuolo, Mariano, La Regina, Giuseppe, Passacantilli, Sara, Grassia, Gianluca, Coluccia, Antonio, La Pietra, Valeria, Giustiniano, Mariateresa, Cassese, Hilde, Di Maro, Salvatore, Brancaccio, Dieg

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 2.87 MB

english, 2015

22

A Binding Mode Hypothesis of Tiagabine Confirms Liothyronine Effect on γ-Aminobutyric Acid Transporter 1 (GAT1)

Jurik, Andreas, Zdrazil, Barbara, Holy, Marion, Stockner, Thomas, Sitte, Harald H., Ecker, Gerhard F.

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 2.34 MB

english, 2015

23

Structure Diversification of Vancomycin through Peptide-Catalyzed, Site-Selective Lipidation: A Catalysis-Based Approach To Combat Glycopeptide-Resistant Pathogens

Yoganathan, Sabesan, Miller, Scott J.

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 1.32 MB

english, 2015

24

Quantum Chemistry Calculation-Aided Structural Optimization of Combretastatin A-4-like Tubulin Polymerization Inhibitors: Improved Stability and Biological Activity

Jiang, Junhang, Zheng, Canhui, Zhu, Kongkai, Liu, Jia, Sun, Nannan, Wang, Chongqing, Jiang, Hualiang, Zhu, Ju, Luo, Cheng, Zhou, Youjun

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 701 KB

english, 2015

25

PAINS in the Assay: Chemical Mechanisms of Assay Interference and Promiscuous Enzymatic Inhibition Observed during a Sulfhydryl-Scavenging HTS

Dahlin, Jayme L., Nissink, J. Willem M., Strasser, Jessica M., Francis, Subhashree, Higgins, LeeAnn, Zhou, Hui, Zhang, Zhiguo, Walters, Michael A.

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 5.41 MB

english, 2015

26

Stabilization of G-Quadruplex DNA, Inhibition of Telomerase Activity, and Tumor Cell Apoptosis by Organoplatinum(II) Complexes with Oxoisoaporphine

Chen, Zhen-Feng, Qin, Qi-Pin, Qin, Jiao-Lan, Liu, Yan-Cheng, Huang, Ke-Bin, Li, Yu-Lan, Meng, Ting, Zhang, Guo-Hai, Peng, Yan, Luo, Xu-Jian, Liang, Hong

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 3.23 MB

english, 2015

27

Discovery of AZD3147: A Potent, Selective Dual Inhibitor of mTORC1 and mTORC2

Pike, Kurt G., Morris, Jeff, Ruston, Linette, Pass, Sarah L., Greenwood, Ryan, Williams, Emma J., Demeritt, Julie, Culshaw, Janet D., Gill, Kristy, Pass, Martin, Finlay, M. Raymond V., Good, Catherine

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 2.75 MB

english, 2015

28

Design, Synthesis, and Biological Evaluation of Novel Matrix Metalloproteinase Inhibitors As Potent Antihemorrhagic Agents: From Hit Identification to an Optimized Lead

Orbe, Josune, Sánchez-Arias, Juan A., Rabal, Obdulia, Rodríguez, José A., Salicio, Agustina, Ugarte, Ana, Belzunce, Miriam, Xu, Musheng, Wu, Wei, Tan, Haizhong, Ma, Hongyu, Páramo, José A., Oyarzabal,

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 1.48 MB

english, 2015

29

Synthesis of CDDO–Amino Acid–Nitric Oxide Donor Trihybrids as Potential Antitumor Agents against Both Drug-Sensitive and Drug-Resistant Colon Cancer

Ai, Yong, Kang, Fenghua, Huang, Zhangjian, Xue, Xiaowen, Lai, Yisheng, Peng, Sixun, Tian, Jide, Zhang, Yihua

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 1.50 MB

english, 2015

30

Synthesis and Biological Evaluation of Indolyl-Pyridinyl-Propenones Having Either Methuosis or Microtubule Disruption Activity

Trabbic, Christopher J., Overmeyer, Jean H., Alexander, Evan M., Crissman, Emily J., Kvale, Heather M., Smith, Marcie A., Erhardt, Paul W., Maltese, William A.

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 3.58 MB

english, 2015

31

5′- C -Ethyl-tetrazolyl- N 6 -Substituted Adenosine and 2-Chloro-adenosine Derivatives as Highly Potent Dual Acting A 1 Adenosine Receptor Agonists and A 3 Adenosine Receptor Antagonists

Petrelli, Riccardo, Torquati, Ilaria, Kachler, Sonja, Luongo, Livio, Maione, Sabatino, Franchetti, Palmarisa, Grifantini, Mario, Novellino, Ettore, Lavecchia, Antonio, Klotz, Karl-Norbert, Cappellacci

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 4.85 MB

english, 2015

32

Small Molecule Binding Sites on the Ras:SOS Complex Can Be Exploited for Inhibition of Ras Activation

Winter, Jon J. G., Anderson, Malcolm, Blades, Kevin, Brassington, Claire, Breeze, Alexander L., Chresta, Christine, Embrey, Kevin, Fairley, Gary, Faulder, Paul, Finlay, M. Raymond V., Kettle, Jason G.

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 9.61 MB

english, 2015

33

Phthalocyanine Derivatives Possessing 2-(Morpholin-4-yl)ethoxy Groups As Potential Agents for Photodynamic Therapy

Kucinska, Malgorzata, Skupin-Mrugalska, Paulina, Szczolko, Wojciech, Sobotta, Lukasz, Sciepura, Mateusz, Tykarska, Ewa, Wierzchowski, Marcin, Teubert, Anna, Fedoruk-Wyszomirska, Agnieszka, Wyszko, Eli

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 3.95 MB

english, 2015

34

Learning from PAINful lessons

Erlanson, Daniel A.

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 323 KB

english, 2015

35

Discovery of Potent and Selective 8-Fluorotriazolopyridine c-Met Inhibitors

Peterson, Emily A., Teffera, Yohannes, Albrecht, Brian K., Bauer, David, Bellon, Steven F., Boezio, Alessandro, Boezio, Christiane, Broome, Martin A., Choquette, Deborah, Copeland, Katrina W., Dussaul

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 2.23 MB

english, 2015

36

Novel Pyridyl Substituted 4,5-Dihydro-[1,2,4]triazolo[4,3- a ]quinolines as Potent and Selective Aldosterone Synthase Inhibitors with Improved in Vitro Metabolic Stability

Hu, Qingzhong, Yin, Lina, Ali, Amjad, Cooke, Andrew J., Bennett, Jonathan, Ratcliffe, Paul, Lo, Michael Man-Chu, Metzger, Edward, Hoyt, Scott, Hartmann, Rolf W.

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 2.55 MB

english, 2015

37

Structure Enabled Design of BAZ2-ICR, A Chemical Probe Targeting the Bromodomains of BAZ2A and BAZ2B

Drouin, Ludovic, McGrath, Sally, Vidler, Lewis R., Chaikuad, Apirat, Monteiro, Octovia, Tallant, Cynthia, Philpott, Martin, Rogers, Catherine, Fedorov, Oleg, Liu, Manjuan, Akhtar, Wasim, Hayes, Angela

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 385 KB

english, 2015

38

Identification of the Molecular Basis of Inhibitor Selectivity between the Human and Streptococcal Type I Methionine Aminopeptidases

Arya, Tarun, Reddi, Ravikumar, Kishor, Chandan, Ganji, Roopa Jones, Bhukya, Supriya, Gumpena, Rajesh, McGowan, Sheena, Drag, Marcin, Addlagatta, Anthony

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 4.97 MB

english, 2015

39

Correction to Tetra -Substituted Pyridinylimidazoles As Dual Inhibitors of p38α Mitogen-Activated Protein Kinase and c-Jun N -Terminal Kinase 3 for Potential Treatment of Neurodegenerative Diseases

Muth, Felix, Günther, Marcel, Bauer, Silke M., Döring, Eva, Fischer, Sabine, Maier, Julia, Drückes, Peter, Köppler, Jürgen, Trappe, Jörg, Rothbauer, Ulrich, Koch, Pierre, Laufer, Stefan A.

Journal:

Journal of Medicinal Chemistry

Year:

2015

File:

PDF, 486 KB

2015

40

Development of a Novel Class of Tubulin Inhibitor from Desmosdumotin B with a Hydroxylated Bicyclic B-Ring

Nakagawa-Goto, Kyoko, Oda, Akifumi, Hamel, Ernest, Ohkoshi, Emika, Lee, Kuo-Hsiung, Goto, Masuo

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 7.82 MB

english, 2015

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