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Volume 52; Issue 22

Journal of Medicinal Chemistry

Volume 52; Issue 22

1

(1-(4-(Naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamine: A Wingless β-Catenin Agonist That Increases Bone Formation Rate

Pelletier, Jeffrey C., Lundquist, Joseph T., Gilbert, Adam M., Alon, Nipa, Bex, Frederick J., Bhat, Bheem M., Bursavich, Mattew G., Coleburn, Valerie E., Felix, Luciana A., Green, Daniel M.

Journal:

Journal of Medicinal Chemistry

Année:

2009

Langue:

english

Fichier:

PDF, 1.53 MB

english, 2009

2

Synthesis and Evaluation of Antiallodynic and Anticonvulsant Activity of Novel Amide and Urea Derivatives of Valproic Acid Analogues

Kaufmann, Dan, Bialer, Meir, Shimshoni, Jakob Avi, Devor, Marshall, Yagen, Boris

Journal:

Journal of Medicinal Chemistry

Année:

2009

Langue:

english

Fichier:

PDF, 999 KB

english, 2009

3

Biaryl Ethers as Novel Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Key Mutant Viruses

Su, Dai-Shi, Lim, John J., Tinney, Elizabeth, Wan, Bang-Lin, Young, Mary Beth, Anderson, Kenneth D., Rudd, Deanne, Munshi, Vandna, Bahnck, Carolyn, Felock, Peter J.

Journal:

Journal of Medicinal Chemistry

Année:

2009

Langue:

english

Fichier:

PDF, 1.06 MB

english, 2009

4

Reactivity of 6-Halopurine Analogs with Glutathione as a Radiotracer for Assessing Function of Multidrug Resistance-Associated Protein 1

Okamura, Toshimitsu, Kikuchi, Tatsuya, Fukushi, Kiyoshi, Irie, Toshiaki

Journal:

Journal of Medicinal Chemistry

Année:

2009

Langue:

english

Fichier:

PDF, 747 KB

english, 2009

5

From Serendipity to Rational Antituberculosis Drug Discovery of Mefloquine-Isoxazole Carboxylic Acid Esters

Pieroni, Marco, Huang, Qingqing, van Breemen, Richard B., Kozikowski, Alan P., Franzblau, Scott G., Wan, Baojie, Mao, Jialin, Yuan, Hai, Wang, Yuehong

Journal:

Journal of Medicinal Chemistry

Année:

2009

Langue:

english

Fichier:

PDF, 1.96 MB

english, 2009

6

Discovery and Optimization of Chromenotriazolopyrimidines as Potent Inhibitors of the Mouse Double Minute 2−Tumor Protein 53 Protein−Protein Interaction

Allen, John G., Bourbeau, Matthew P., Wohlhieter, G. Erich, Bartberger, Michael D., Michelsen, Klaus, Hungate, Randall, Gadwood, Robert C., Gaston, Rick D., Evans, Bruce, Mann, Larry W.

Journal:

Journal of Medicinal Chemistry

Année:

2009

Langue:

english

Fichier:

PDF, 992 KB

english, 2009

7

Synthesis, Structure−Activity Relationships, and Characterization of Novel Nonsteroidal and Selective Androgen Receptor Modulators

Schlienger, Nathalie, Lund, Birgitte W., Pawlas, Jan, Badalassi, Fabrizio, Bertozzi, Fabio, Lewinsky, Rasmus, Fejzic, Alma, Thygesen, Mikkel B., Tabatabaei, Ali, Bradley, Stefania Risso

Journal:

Journal of Medicinal Chemistry

Année:

2009

Langue:

english

Fichier:

PDF, 818 KB

english, 2009

8

Structure−Activity Relationship Studies of Chalcone Leading to 3-Hydroxy-4,3′,4′,5′-tetramethoxychalcone and Its Analogues as Potent Nuclear Factor κB Inhibitors and Their Anticancer Activities

Srinivasan, Balasubramanian, Johnson, Thomas E., Lad, Rahul, Xing, Chengguo

Journal:

Journal of Medicinal Chemistry

Année:

2009

Langue:

english

Fichier:

PDF, 1.01 MB

english, 2009

9

Neuroprotective and Cholinergic Properties of Multifunctional Glutamic Acid Derivatives for the Treatment of Alzheimer’s Disease

Arce, Mariana P., Rodríguez-Franco, María Isabel, González-Muñoz, Gema C., Pérez, Concepción, López, Beatriz, Villarroya, Mercedes, López, Manuela G., García, Antonio G., Conde, Santiago

Journal:

Journal of Medicinal Chemistry

Année:

2009

Langue:

english

Fichier:

PDF, 801 KB

english, 2009

10

Design of HIV Protease Inhibitors Based on Inorganic Polyhedral Metallacarboranes

Řezáčová, Pavlína, Pokorná, Jana, Brynda, Jiří, Kožíšek, Milan, Cígler, Petr, Lepšík, Martin, Fanfrlík, Jindřich, Řezáč, Jan, Grantz Šašková, Klára, Sieglová, Irena, Plešek, J

Journal:

Journal of Medicinal Chemistry

Année:

2009

Langue:

english

Fichier:

PDF, 4.38 MB

english, 2009

11

Novel Compounds Designed as Antistress Agents

Tsiakitzis, Karyophyllis C., Rekka, Eleni A., Kourounakis, Angeliki P., Kourounakis, Panos N.

Journal:

Journal of Medicinal Chemistry

Année:

2009

Langue:

english

Fichier:

PDF, 697 KB

english, 2009

12

Synthesis, Crystallization, and Biological Evaluation of an Orally Active Prodrug of Gemcitabine

Bender, David M., Bao, Jingqi, Dantzig, Anne H., Diseroad, William D., Law, Kevin L., Magnus, Nicholas A., Peterson, Jeffrey A., Perkins, Everett J., Pu, Yangwei J., Reutzel-Edens, Susan M., Remick, D

Journal:

Journal of Medicinal Chemistry

Année:

2009

Langue:

english

Fichier:

PDF, 952 KB

english, 2009

13

α v β 3 Integrin-Targeting Arg-Gly-Asp (RGD) Peptidomimetics Containing Oligoethylene Glycol (OEG) Spacers

Rerat, Vincent, Dive, Georges, Cordi, Alex A., Tucker, Gordon C., Bareille, Reine, Amédée, Joëlle, Bordenave, Laurence, Marchand-Brynaert, Jacqueline

Journal:

Journal of Medicinal Chemistry

Année:

2009

Langue:

english

Fichier:

PDF, 3.08 MB

english, 2009

14

Discovery of 2-{4-[(3 S )-Piperidin-3-yl]phenyl}-2 H -indazole-7-carboxamide (MK-4827): A Novel Oral Poly(ADP-ribose)polymerase (PARP) Inhibitor Efficacious in BRCA-1 and -2 Mutant Tumors

Jones, Philip, Altamura, Sergio, Boueres, Julia, Ferrigno, Federica, Fonsi, Massimiliano, Giomini, Claudia, Lamartina, Stefania, Monteagudo, Edith, Ontoria, Jesus M., Orsale, Maria Vittoria, Palumbi,

Journal:

Journal of Medicinal Chemistry

Année:

2009

Langue:

english

Fichier:

PDF, 1.79 MB

english, 2009

15

Synthesis and Biological Evaluation of Coumarin-Based Inhibitors of NAD(P)H: Quinone Oxidoreductase-1 (NQO1) †

Nolan, Karen A., Doncaster, Jeremy R., Dunstan, Mark S., Scott, Katherine A., Frenkel, A. David, Siegel, David, Ross, David, Barnes, John, Levy, Colin, Leys, David, Whitehead, Roger C., Stratford, Ian

Journal:

Journal of Medicinal Chemistry

Année:

2009

Langue:

english

Fichier:

PDF, 4.66 MB

english, 2009

16

Asymmetrical Diaromatic Guanidinium/2-Aminoimidazolinium Derivatives: Synthesis and DNA Affinity

Nagle, Padraic S., Rodriguez, Fernando, Kahvedžić, Amila, Quinn, Susan J., Rozas, Isabel

Journal:

Journal of Medicinal Chemistry

Année:

2009

Langue:

english

Fichier:

PDF, 1.08 MB

english, 2009

17

Bis(dialkylaminethiocarbonyl)disulfides as Potent and Selective Monoglyceride Lipase Inhibitors

Kapanda, Coco N., Muccioli, Giulio G., Labar, Geoffray, Poupaert, Jacques H., Lambert, Didier M.

Journal:

Journal of Medicinal Chemistry

Année:

2009

Langue:

english

Fichier:

PDF, 972 KB

english, 2009

18

Aza-Peptidyl Michael Acceptor and Epoxide Inhibitors—Potent and Selective Inhibitors of Schistosoma mansoni and Ixodes ricinus Legumains (Asparaginyl Endopeptidases)

Ovat, Asli, Muindi, Fanuel, Fagan, Crystal, Brouner, Michelle, Hansell, Elizabeth, Dvořák, Jan, Sojka, Daniel, Kopáček, Petr, McKerrow, James H., Caffrey, Conor R., Powers, James C.

Journal:

Journal of Medicinal Chemistry

Année:

2009

Langue:

english

Fichier:

PDF, 1.09 MB

english, 2009

19

4-Pregnen-21-ol-3,20-dione-21-(4-bromobenzenesufonate) (NSC 88915) and Related Novel Steroid Derivatives as Tyrosyl-DNA Phosphodiesterase (Tdp1) Inhibitors

Dexheimer, Thomas S., Gediya, Lalji K., Stephen, Andrew G., Weidlich, Iwona, Antony, Smitha, Marchand, Christophe, Interthal, Heidrun, Nicklaus, Marc, Fisher, Robert J., Njar, Vincent C., Pommier, Yve

Journal:

Journal of Medicinal Chemistry

Année:

2009

Langue:

english

Fichier:

PDF, 2.26 MB

english, 2009

20

Synthesis and Evaluation of Three 18 F-Labeled Aminophenylbenzothiazoles as Amyloid Imaging Agents

Serdons, Kim, Van Laere, Koen, Janssen, Peter, Kung, Hank F., Bormans, Guy, Verbruggen, Alfons

Journal:

Journal of Medicinal Chemistry

Année:

2009

Langue:

english

Fichier:

PDF, 4.50 MB

english, 2009

21

Discovery of Potent and Selective Inhibitors of the Mammalian Target of Rapamycin (mTOR) Kinase

Nowak, Pawel, Cole, Derek C., Brooijmans, Natasja, Bursavich, Matthew G., Curran, Kevin J., Ellingboe, John W., Gibbons, James J., Hollander, Irwin, Hu, YongBo, Kaplan, Joshua, Malwitz, David J., Tora

Journal:

Journal of Medicinal Chemistry

Année:

2009

Langue:

english

Fichier:

PDF, 1.90 MB

english, 2009

22

The Synthesis of Haptens and Their Use for the Development of Monoclonal Antibodies for Treating Methamphetamine Abuse

Carroll, F. Ivy, Abraham, Philip, Gong, Paul K., Pidaparthi, Ramakrishna R., Blough, Bruce E., Che, Yingni, Hampton, Amber, Gunnell, Melinda, Lay, Jackson O., Peterson, Eric C., Owens, S. Michael

Journal:

Journal of Medicinal Chemistry

Année:

2009

Langue:

english

Fichier:

PDF, 935 KB

english, 2009

23

Synthetic mRNA Splicing Modulator Compounds with in Vivo Antitumor Activity

Lagisetti, Chandraiah, Pourpak, Alan, Goronga, Tinopiwa, Jiang, Qin, Cui, Xiaoli, Hyle, Judith, Lahti, Jill M., Morris, Stephan W., Webb, Thomas R.

Journal:

Journal of Medicinal Chemistry

Année:

2009

Langue:

english

Fichier:

PDF, 3.20 MB

english, 2009

24

Azaindole Hydroxamic Acids are Potent HIV-1 Integrase Inhibitors

Plewe, Michael B., Butler, Scott L., R. Dress, Klaus, Hu, Qiyue, Johnson, Ted W., Kuehler, Jon E., Kuki, Atsuo, Lam, Hieu, Liu, Wen, Nowlin, Dawn, Peng, Qinghai, Rahavendran, Sadayappan V., Tanis, Ste

Journal:

Journal of Medicinal Chemistry

Année:

2009

Langue:

english

Fichier:

PDF, 863 KB

english, 2009

25

Inhibitors for Human Glutaminyl Cyclase by Structure Based Design and Bioisosteric Replacement

Buchholz, Mirko, Hamann, Antje, Aust, Susanne, Brandt, Wolfgang, Böhme, Livia, Hoffmann, Torsten, Schilling, Stephan, Demuth, Hans-Ulrich, Heiser, Ulrich

Journal:

Journal of Medicinal Chemistry

Année:

2009

Langue:

english

Fichier:

PDF, 2.24 MB

english, 2009

26

Microtubule-Stabilizing Activity of Zampanolide, a Potent Macrolide Isolated from the Tongan Marine Sponge Cacospongia mycofijiensis

Field, Jessica J., Singh, A. Jonathan, Kanakkanthara, Arun, Halafihi, Tu’ikolongahau, Northcote, Peter T., Miller, John H.

Journal:

Journal of Medicinal Chemistry

Année:

2009

Langue:

english

Fichier:

PDF, 2.39 MB

english, 2009

27

The Role of Membranes in the Organization of HIV-1 Gag p6 and Vpr: p6 Shows High Affinity for Membrane Bilayers Which Substantially Increases the Interaction between p6 and Vpr.

Salgado, Gilmar F., Vogel, Alexander, Marquant, Rodrigue, Feller, Scott E., Bouaziz, Serge, Alves, Isabel D.

Journal:

Journal of Medicinal Chemistry

Année:

2009

Langue:

english

Fichier:

PDF, 2.62 MB

english, 2009

28

χ-Conopeptide Pharmacophore Development: Toward a Novel Class of Norepinephrine Transporter Inhibitor (Xen2174) for Pain ⊥

Brust, Andreas, Palant, Elka, Croker, Daniel E., Colless, Barbara, Drinkwater, Roger, Patterson, Brad, Schroeder, Christina I., Wilson, David, Nielsen, Carsten K., Smith, Maree T., Alewood, Dianne, Al

Journal:

Journal of Medicinal Chemistry

Année:

2009

Langue:

english

Fichier:

PDF, 3.79 MB

english, 2009

29

Hypoxia-Activated Prodrugs: Substituent Effects on the Properties of Nitro seco -1,2,9,9a-Tetrahydrocyclopropa[ c ]benz[ e ]indol-4-one (nitroCBI) Prodrugs of DNA Minor Groove Alkylating Agents

Tercel, Moana, Atwell, Graham J., Yang, Shangjin, Stevenson, Ralph J., Botting, K. Jane, Boyd, Maruta, Smith, Eileen, Anderson, Robert F., Denny, William A., Wilson, William R., Pruijn, Frederik B.

Journal:

Journal of Medicinal Chemistry

Année:

2009

Langue:

english

Fichier:

PDF, 1.64 MB

english, 2009

30

Discovery of Novel Benzoxazinones as Potent and Orally Active Long Chain Fatty Acid Elongase 6 Inhibitors

Mizutani, Takashi, Ishikawa, Shiho, Nagase, Tsuyoshi, Takahashi, Hidekazu, Fujimura, Takashi, Sasaki, Takahide, Nagumo, Akira, Shimamura, Ken, Miyamoto, Yasuhisa, Kitazawa, Hidefumi, Kanesaka, Maki, Y

Journal:

Journal of Medicinal Chemistry

Année:

2009

Langue:

english

Fichier:

PDF, 953 KB

english, 2009

31

Novel Macrocyclic Inhibitors of Hepatitis C NS3/4A Protease Featuring a 2-Amino-1,3-thiazole as a P4 Carbamate Replacement

Di Francesco, M. Emilia, Dessole, Gabriella, Nizi, Emanuela, Pace, Paola, Koch, Uwe, Fiore, Fabrizio, Pesci, Silvia, Di Muzio, Jillian, Monteagudo, Edith, Rowley, Michael, Summa, Vincenzo

Journal:

Journal of Medicinal Chemistry

Année:

2009

Langue:

english

Fichier:

PDF, 2.49 MB

english, 2009

32

Binding Ensemble Profiling with Photoaffinity Labeling (BEProFL) Approach: Mapping the Binding Poses of HDAC8 Inhibitors

He, Bai, Velaparthi, Subash, Pieffet, Gilles, Pennington, Chris, Mahesh, Aruna, Holzle, Denise L., Brunsteiner, Michael, van Breemen, Richard, Blond, Sylvie Y., Petukhov, Pavel A.

Journal:

Journal of Medicinal Chemistry

Année:

2009

Langue:

english

Fichier:

PDF, 2.81 MB

english, 2009

33

Identification of Death-Associated Protein Kinases Inhibitors Using Structure-Based Virtual Screening

Okamoto, Masako, Takayama, Kiyoshi, Shimizu, Tomoko, Ishida, Kazuhiro, Takahashi, Osamu, Furuya, Toshio

Journal:

Journal of Medicinal Chemistry

Année:

2009

Langue:

english

Fichier:

PDF, 1.78 MB

english, 2009

34

Identification of a Critical Residue in the Transmembrane Domain 2 of Tachykinin Neurokinin 3 Receptor Affecting the Dissociation Kinetics and Antagonism Mode of Osanetant (SR 142801) and Piperidine-Based Structures

Malherbe, Pari, Kratzeisen, Claudia, Marcuz, Anne, Zenner, Marie-Thérèse, Nettekoven, Matthias H., Ratni, Hasane, Wettstein, Joseph G., Bissantz, Caterina

Journal:

Journal of Medicinal Chemistry

Année:

2009

Langue:

english

Fichier:

PDF, 2.89 MB

english, 2009

35

β-Lactams Derived from a Carbapenem Chiron Are Selective Inhibitors of Human Fatty Acid Amide Hydrolase versus Human Monoacylglycerol Lipase

Feledziak, Marion, Michaux, Catherine, Urbach, Allan, Labar, Geoffray, Muccioli, Giulio G., Lambert, Didier M., Marchand-Brynaert, Jacqueline

Journal:

Journal of Medicinal Chemistry

Année:

2009

Langue:

english

Fichier:

PDF, 3.57 MB

english, 2009

36

A Novel Manganese Complex Effective as Superoxide Anion Scavenger and Therapeutic Agent against Cell and Tissue Oxidative Injury

Failli, Paola, Bani, Daniele, Bencini, Andrea, Cantore, Miriam, Di Cesare Mannelli, Lorenzo, Ghelardini, Carla, Giorgi, Claudia, Innocenti, Massimo, Rugi, Francesco, Spepi, Alessio, Udisti, Roberto, V

Journal:

Journal of Medicinal Chemistry

Année:

2009

Langue:

english

Fichier:

PDF, 1.13 MB

english, 2009

37

Losartan-Antioxidant Hybrids: Novel Molecules for the Prevention of Hypertension-Induced Cardiovascular Damage

García, Gonzalo, Rodríguez-Puyol, Manuel, Alajarín, Ramón, Serrano, Isabel, Sánchez-Alonso, Patricia, Griera, Mercedes, Vaquero, Juan J., Rodríguez-Puyol, Diego, Álvarez-Builla, Julio, Díez-Ma

Journal:

Journal of Medicinal Chemistry

Année:

2009

Langue:

english

Fichier:

PDF, 1.26 MB

english, 2009

38

Might Adrenergic α 2C -Agonists/α 2A -Antagonists Become Novel Therapeutic Tools for Pain Treatment with Morphine?(1)

Cardinaletti, Claudia, Mattioli, Laura, Ghelfi, Francesca, Del Bello, Fabio, Giannella, Mario, Bruzzone, Ariana, Paris, Hervé, Perfumi, Marina, Piergentili, Alessandro, Quaglia, Wilma, Pigini, Maria

Journal:

Journal of Medicinal Chemistry

Année:

2009

Langue:

english

Fichier:

PDF, 1.00 MB

english, 2009

39

Exploring Chemical Space with Aptamers

Famulok, Michael

Journal:

Journal of Medicinal Chemistry

Année:

2009

Langue:

english

Fichier:

PDF, 2.24 MB

english, 2009