Campagne de collecte 15 septembre 2024 – 1 octobre 2024 C'est quoi, la collecte de fonds?

Volume 56; Issue 6

Journal of Medicinal Chemistry

Volume 56; Issue 6

1

Structure-Based Discovery of Pyrazolobenzothiazine Derivatives As Inhibitors of Hepatitis C Virus Replication

Barreca, Maria Letizia, Manfroni, Giuseppe, Leyssen, Pieter, Winquist, Johan, Kaushik-Basu, Neerja, Paeshuyse, Jan, Krishnan, Ramalingam, Iraci, Nunzio, Sabatini, Stefano, Tabarrini, Oriana, Basu, Ama

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 826 KB

english, 2013

2

A Novel Class of Oral Direct Renin Inhibitors: Highly Potent 3,5-Disubstituted Piperidines Bearing a Tricyclic P 3– P 1 Pharmacophore

Ostermann, Nils, Ruedisser, Simon, Ehrhardt, Claus, Breitenstein, Werner, Marzinzik, Andreas, Jacoby, Edgar, Vangrevelinghe, Eric, Ottl, Johannes, Klumpp, Martin, Hartwieg, J. Constanze D., Cumin, Fre

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 851 KB

english, 2013

3

Discovery of a Novel Class of Highly Potent, Selective, ATP-Competitive, and Orally Bioavailable Inhibitors of the Mammalian Target of Rapamycin (mTOR)

Takeuchi, Craig S., Kim, Byung Gyu, Blazey, Charles M., Ma, Sunghoon, Johnson, Henry W. B., Anand, Neel K., Arcalas, Arlyn, Baik, Tae Gon, Buhr, Chris A., Cannoy, Jonah, Epshteyn, Sergey, Joshi, Anagh

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 4.36 MB

english, 2013

4

Exploring a New Frontier in Cancer Treatment: Targeting the Ubiquitin and Ubiquitin-like Activating Enzymes

da Silva, Sara R., Paiva, Stacey-Lynn, Lukkarila, Julie L., Gunning, Patrick T.

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 1.71 MB

english, 2013

5

Quantum Mechanics/Molecular Mechanics Modeling of Fatty Acid Amide Hydrolase Reactivation Distinguishes Substrate from Irreversible Covalent Inhibitors

Lodola, Alessio, Capoferri, Luigi, Rivara, Silvia, Tarzia, Giorgio, Piomelli, Daniele, Mulholland, Adrian, Mor, Marco

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 668 KB

english, 2013

6

Evaluation of Difluoromethyl Ketones as Agonists of the γ-Aminobutyric Acid Type B (GABA B ) Receptor

Han, Changho, Salyer, Amy E., Kim, Eun Hoo, Jiang, Xinyi, Jarrard, Rachel E., Powers, Matthew S., Kirchhoff, Aaron M., Salvador, Tolani K., Chester, Julia A., Hockerman, Gregory H., Colby, David A.

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 1.01 MB

english, 2013

7

Design and Synthesis of New Bifunctional Sigma-1 Selective Ligands with Antioxidant Activity

Prezzavento, O., Arena, E., Parenti, C., Pasquinucci, L., Aricò, G., Scoto, G. M., Grancara, S., Toninello, A., Ronsisvalle, S.

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 696 KB

english, 2013

8

Colloidal Aggregation Causes Inhibition of G Protein-Coupled Receptors

Sassano, Maria F., Doak, Allison K., Roth, Bryan L., Shoichet, Brian K.

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 408 KB

english, 2013

9

How Are Fragments Optimized? A Retrospective Analysis of 145 Fragment Optimizations

Ferenczy, György G., Keserű, György M.

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 478 KB

english, 2013

10

Antitrypanosomal Lead Discovery: Identification of a Ligand-Efficient Inhibitor of Trypanosoma cruzi CYP51 and Parasite Growth

Andriani, Grasiella, Amata, Emanuele, Beatty, Joel, Clements, Zeke, Coffey, Brian J., Courtemanche, Gilles, Devine, William, Erath, Jessey, Juda, Cristin E., Wawrzak, Zdzislaw, Wood, JodiAnne T., Lepe

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 505 KB

english, 2013

11

Synthesis and Antimalarial Efficacy of Two-Carbon-Linked, Artemisinin-Derived Trioxane Dimers in Combination with Known Antimalarial Drugs

Mott, Bryan T., Tripathi, Abhai, Siegler, Maxime A., Moore, Cathy D., Sullivan, David J., Posner, Gary H.

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 523 KB

english, 2013

12

Development of Dual PLD1/2 and PLD2 Selective Inhibitors from a Common 1,3,8-Triazaspiro[4.5]decane Core: Discovery of ML298 and ML299 That Decrease Invasive Migration in U87-MG Glioblastoma Cells

O’Reilly, Matthew C., Scott, Sarah A., Brown, Kyle A., Oguin, Thomas H., Thomas, Paul G., Daniels, J. Scott, Morrison, Ryan, Brown, H. Alex, Lindsley, Craig W.

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 803 KB

english, 2013

13

2-Arylpyrazolo[4,3- d ]pyrimidin-7-amino Derivatives As New Potent and Selective Human A 3 Adenosine Receptor Antagonists. Molecular Modeling Studies and Pharmacological Evaluation

Squarcialupi, Lucia, Colotta, Vittoria, Catarzi, Daniela, Varano, Flavia, Filacchioni, Guido, Varani, Katia, Corciulo, Carmen, Vincenzi, Fabrizio, Borea, Pier Andrea, Ghelardini, Carla, Di Cesare Mann

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 2.38 MB

english, 2013

14

Acyclic Nucleoside Phosphonates Containing a Second Phosphonate Group Are Potent Inhibitors of 6-Oxopurine Phosphoribosyltransferases and Have Antimalarial Activity

Keough, Dianne T., Špaček, Petr, Hocková, Dana, Tichý, Tomáš, Vrbková, Silvie, Slavětínská, Lenka, Janeba, Zlatko, Naesens, Lieve, Edstein, Michael D., Chavchich, Marina, Wang, Tzu-Hsuan, de Jersey, J

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 712 KB

english, 2013

15

Comparative Antimalarial Activities and ADME Profiles of Ozonides (1,2,4-trioxolanes) OZ277, OZ439, and Their 1,2-Dioxolane, 1,2,4-Trioxane, and 1,2,4,5-Tetraoxane Isosteres

Wang, Xiaofang, Dong, Yuxiang, Wittlin, Sergio, Charman, Susan A., Chiu, Francis C. K., Chollet, Jacques, Katneni, Kasiram, Mannila, Janne, Morizzi, Julia, Ryan, Eileen, Scheurer, Christian, Steuten,

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 534 KB

english, 2013

16

A New Target for an Old Drug: Identifying Mitoxantrone as a Nanomolar Inhibitor of PIM1 Kinase via Kinome-Wide Selectivity Modeling

Wan, Xiaobo, Zhang, Wei, Li, Li, Xie, Yuting, Li, Wei, Huang, Niu

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 3.17 MB

english, 2013

17

Fragment-Based Discovery of 8-Hydroxyquinoline Inhibitors of the HIV-1 Integrase–Lens Epithelium-Derived Growth Factor/p75 (IN–LEDGF/p75) Interaction

Serrao, Erik, Debnath, Bikash, Otake, Hiroyuki, Kuang, Yuting, Christ, Frauke, Debyser, Zeger, Neamati, Nouri

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 3.24 MB

english, 2013

18

Discovery of Allosteric Modulators of Factor XIa by Targeting Hydrophobic Domains Adjacent to Its Heparin-Binding Site

Karuturi, Rajesh, Al-Horani, Rami A., Mehta, Shrenik C., Gailani, David, Desai, Umesh R.

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 1.49 MB

english, 2013

19

Optimization of Peptide Hydroxamate Inhibitors of Insulin-Degrading Enzyme Reveals Marked Substrate-Selectivity

Abdul-Hay, Samer O., Lane, Amy L., Caulfield, Thomas R., Claussin, Clémence, Bertrand, Juliette, Masson, Amandine, Choudhry, Shakeel, Fauq, Abdul H., Maharvi, Guhlam M., Leissring, Malcolm A.

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 2.63 MB

english, 2013

20

Synthesis and Biological Evaluation of 2-(Alkoxycarbonyl)-3-Anilinobenzo[ b ]thiophenes and Thieno[2,3- b ]pyridines as New Potent Anticancer Agents

Romagnoli, Romeo, Baraldi, Pier Giovanni, Kimatrai Salvador, Maria, Preti, Delia, Aghazadeh Tabrizi, Mojgan, Bassetto, Marcella, Brancale, Andrea, Hamel, Ernest, Castagliuolo, Ignazio, Bortolozzi, Rob

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 2.84 MB

english, 2013

21

The Development of Highly Potent Inhibitors for Porcupine

Wang, Xiaolei, Moon, Jesung, Dodge, Michael E., Pan, Xinchao, Zhang, Lishu, Hanson, Jordan M., Tuladhar, Rubina, Ma, Zhiqiang, Shi, Heping, Williams, Noelle S., Amatruda, James F., Carroll, Thomas J.,

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 2.10 MB

english, 2013

22

Design, Synthesis, and Biological Evaluation of Highly Potent Small Molecule–Peptide Conjugates as New HIV-1 Fusion Inhibitors

Wang, Chao, Shi, Weiguo, Cai, Lifeng, Lu, Lu, Wang, Qian, Zhang, Tianhong, Li, Jinglai, Zhang, Zhenqing, Wang, Kun, Xu, Liang, Jiang, Xifeng, Jiang, Shibo, Liu, Keliang

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 3.30 MB

english, 2013

23

Development of κ Opioid Receptor Antagonists

Carroll, F. Ivy, Carlezon, William A.

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 635 KB

english, 2013

24

The Discovery of Novel Potent trans -3,4-Disubstituted Pyrrolidine Inhibitors of the Human Aspartic Protease Renin from in Silico Three-Dimensional (3D) Pharmacophore Searches

Lorthiois, Edwige, Breitenstein, Werner, Cumin, Frederic, Ehrhardt, Claus, Francotte, Eric, Jacoby, Edgar, Ostermann, Nils, Sellner, Holger, Kosaka, Takatoshi, Webb, Randy L., Rigel, Dean F., Hassiepe

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 1.18 MB

english, 2013

25

Antimalarial Activities of 6-Iodouridine and Its Prodrugs and Potential for Combination Therapy

Crandall, Ian E., Wasilewski, Ewa, Bello, Angelica M., Mohmmed, Asif, Malhotra, Pawan, Pai, Emil F., Kain, Kevin C., Kotra, Lakshmi P.

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 758 KB

english, 2013

26

Discovery of 1-[3-(1-Methyl-1 H -pyrazol-4-yl)-5-oxo-5 H -benzo[4,5]cyclohepta[1,2- b ]pyridin-7-yl]- N -(pyridin-2-ylmethyl)methanesulfonamide (MK-8033): A Specific c-Met/Ron Dual Kinase Inhibitor with Preferential Affinity for the Activated State of c-Met

Northrup, Alan B., Katcher, Matthew H., Altman, Michael D., Chenard, Melissa, Daniels, Matthew H., Deshmukh, Sujal V., Falcone, Danielle, Guerin, David J., Hatch, Harold, Li, Chaomin, Lu, Wei, Lutterb

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 3.01 MB

english, 2013

27

Gastrin Releasing Peptide Receptor-Directed Radioligands Based on a Bombesin Antagonist: Synthesis, 111 In-Labeling, and Preclinical Profile

Marsouvanidis, Panteleimon J., Nock, Berthold A., Hajjaj, Bouchra, Fehrentz, Jean-Alain, Brunel, Luc, M’Kadmi, Céline, van der Graaf, Linda, Krenning, Eric P., Maina, Theodosia, Martinez, Jean, de Jon

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 1.40 MB

english, 2013

28

Studies on an ( S )-2-Amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic Acid (AMPA) Receptor Antagonist IKM-159: Asymmetric Synthesis, Neuroactivity, and Structural Characterization

Juknaitė, Lina, Sugamata, Yutaro, Tokiwa, Kazuya, Ishikawa, Yuichi, Takamizawa, Satoshi, Eng, Andrew, Sakai, Ryuichi, Pickering, Darryl S., Frydenvang, Karla, Swanson, Geoffrey T., Kastrup, Jette S.,

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 573 KB

english, 2013

29

Allopregnanolone and Pregnanolone Analogues Modified in the C Ring: Synthesis and Activity

Slavíková, Barbora, Bujons, Jordi, Matyáš, Libor, Vidal, Miguel, Babot, Zoila, Krištofíková, Zdena, Suñol, Cristina, Kasal, Alexander

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 502 KB

english, 2013

30

A Synthetic Dolastatin 10 Analogue Suppresses Microtubule Dynamics, Inhibits Cell Proliferation, and Induces Apoptotic Cell Death

Gajula, Praveen Kumar, Asthana, Jayant, Panda, Dulal, Chakraborty, Tushar Kanti

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 1.70 MB

english, 2013

31

Arylazanylpyrazolone Derivatives as Inhibitors of Mutant Superoxide Dismutase 1 Dependent Protein Aggregation for the Treatment of Amyotrophic Lateral Sclerosis

Zhang, Yinan, Benmohamed, Radhia, Huang, He, Chen, Tian, Voisine, Cindy, Morimoto, Richard I., Kirsch, Donald R., Silverman, Richard B.

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 1.07 MB

english, 2013

32

Design, Synthesis, and Biological Evaluation of Indenoisoquinoline Rexinoids with Chemopreventive Potential

Conda-Sheridan, Martin, Park, Eun-Jung, Beck, Daniel E., Reddy, P. V. Narasimha, Nguyen, Trung X., Hu, Bingjie, Chen, Lian, White, Jerry J., van Breemen, Richard B., Pezzuto, John M., Cushman, Mark

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 955 KB

english, 2013

33

Solubility-Driven Optimization of (Pyridin-3-yl) Benzoxazinyl-oxazolidinones Leading to a Promising Antibacterial Agent

Guo, Bin, Fan, Houxing, Xin, Qisheng, Chu, Wenjing, Wang, Hui, Huang, Yanqin, Chen, Xiaoyan, Yang, Yushe

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 496 KB

english, 2013

34

Synthesis and Preliminary Evaluation in Tumor Bearing Mice of New 18 F-Labeled Arylsulfone Matrix Metalloproteinase Inhibitors as Tracers for Positron Emission Tomography

Casalini, Francesca, Fugazza, Lorenza, Esposito, Giovanna, Cabella, Claudia, Brioschi, Chiara, Cordaro, Alessia, D’Angeli, Luca, Bartoli, Antonietta, Filannino, Azzurra M., Gringeri, Concetta V., Long

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 1.55 MB

english, 2013

35

Synthesis and Relaxometric Characterization of a MRI Gd-Based Probe Responsive to Glutamic Acid Decarboxylase Enzymatic Activity

Napolitano, Roberta, Pariani, Giorgio, Fedeli, Franco, Baranyai, Zsolt, Aswendt, Markus, Aime, Silvio, Gianolio, Eliana

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 2.97 MB

english, 2013

36

Synthesis and Biological Characterization of New Aminophosphonates for Mitochondrial pH Determination by 31 P NMR Spectroscopy

Culcasi, Marcel, Casano, Gilles, Lucchesi, Céline, Mercier, Anne, Clément, Jean-Louis, Pique, Valérie, Michelet, Laure, Krieger-Liszkay, Anja, Robin, Maxime, Pietri, Sylvia

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 1.20 MB

english, 2013

37

Discovery of ( R )-2-Amino-6-borono-2-(2-(piperidin-1-yl)ethyl)hexanoic Acid and Congeners As Highly Potent Inhibitors of Human Arginases I and II for Treatment of Myocardial Reperfusion Injury

Van Zandt, Michael C., Whitehouse, Darren L., Golebiowski, Adam, Ji, Min Koo, Zhang, Mingbao, Beckett, R. Paul, Jagdmann, G. Erik, Ryder, Todd R., Sheeler, Ryan, Andreoli, Monica, Conway, Bruce, Mahbo

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 4.68 MB

english, 2013

38

Non-Nucleoside Inhibitors of BasE, an Adenylating Enzyme in the Siderophore Biosynthetic Pathway of the Opportunistic Pathogen Acinetobacter baumannii

Neres, João, Engelhart, Curtis A., Drake, Eric J., Wilson, Daniel J., Fu, Peng, Boshoff, Helena I., Barry, Clifton E., Gulick, Andrew M., Aldrich, Courtney C.

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 2.12 MB

english, 2013

39

Development of Potent and Selective Indomethacin Analogues for the Inhibition of AKR1C3 (Type 5 17β-Hydroxysteroid Dehydrogenase/Prostaglandin F Synthase) in Castrate-Resistant Prostate Cancer

Liedtke, Andy J., Adeniji, Adegoke O., Chen, Mo, Byrns, Michael C., Jin, Yi, Christianson, David W., Marnett, Lawrence J., Penning, Trevor M.

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 4.03 MB

english, 2013

40

Discovery, Biological Evaluation, and Structure–Activity and −Selectivity Relationships of 6′-Substituted ( E )-2-(Benzofuran-3(2 H )-ylidene)- N -methylacetamides, a Novel Class of Potent and Selective Monoamine Oxidase Inhibitors

Pisani, Leonardo, Barletta, Maria, Soto-Otero, Ramon, Nicolotti, Orazio, Mendez-Alvarez, Estefania, Catto, Marco, Introcaso, Antonellina, Stefanachi, Angela, Cellamare, Saverio, Altomare, Cosimo, Caro

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 1.65 MB

english, 2013

41

Design and Synthesis of Amphiphilic Xanthone-Based, Membrane-Targeting Antimicrobials with Improved Membrane Selectivity

Zou, Hanxun, Koh, Jun-Jie, Li, Jianguo, Qiu, Shengxiang, Aung, Thet Tun, Lin, Huifen, Lakshminarayanan, Rajamani, Dai, Xiaoping, Tang, Charles, Lim, Fang Hui, Zhou, Lei, Tan, Ai Ling, Verma, Chandra,

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 1.76 MB

english, 2013

42

Anticancer Therapy by Tumor Vessel Infarction with Polyethylene Glycol Conjugated Retargeted Tissue Factor

Schwöppe, Christian, Zerbst, Caroline, Fröhlich, Max, Schliemann, Christoph, Kessler, Torsten, Liersch, Ruediger, Overkamp, Laura, Holtmeier, Richard, Stypmann, Jörg, Dreiling, Alena, König, Simone, H

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 1.10 MB

english, 2013

43

Optimizing Solubility and Permeability of a Biopharmaceutics Classification System (BCS) Class 4 Antibiotic Drug Using Lipophilic Fragments Disturbing the Crystal Lattice

Tehler, Ulrika, Fagerberg, Jonas H., Svensson, Richard, Larhed, Mats, Artursson, Per, Bergström, Christel A. S.

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 915 KB

english, 2013

44

Development and Characterization of Monomeric N-End Rule Inhibitors through In Vitro Model Substrates

Sriram, Shashi, Lee, Jung Hoon, Mai, Binh Khanh, Jiang, Yanxialei, Kim, Yongho, Yoo, Young Dong, Banerjee, Rajkumar, Lee, Seung-Han, Lee, Min Jae

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 2.21 MB

english, 2013