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Volume 58; Issue 3

Journal of Medicinal Chemistry

Volume 58; Issue 3

1

Glucagon-like Peptide-1 (GLP-1) Analogs: Recent Advances, New Possibilities, and Therapeutic Implications

Manandhar, Bikash, Ahn, Jung-Mo

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 1.27 MB

english, 2015

2

Small-Molecule Inhibitors of the MDM2–p53 Protein–Protein Interaction (MDM2 Inhibitors) in Clinical Trials for Cancer Treatment

Zhao, Yujun, Aguilar, Angelo, Bernard, Denzil, Wang, Shaomeng

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 7.84 MB

english, 2015

3

Nintedanib: From Discovery to the Clinic

Roth, Gerald J., Binder, Rudolf, Colbatzky, Florian, Dallinger, Claudia, Schlenker-Herceg, Rozsa, Hilberg, Frank, Wollin, Stefan-Lutz, Kaiser, Rolf

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 867 KB

english, 2015

4

Effect of Size and N-Terminal Residue Characteristics on Bacterial Cell Penetration and Antibacterial Activity of the Proline-Rich Peptide Bac7

Guida, Filomena, Benincasa, Monica, Zahariev, Sotir, Scocchi, Marco, Berti, Federico, Gennaro, Renato, Tossi, Alessandro

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 1.89 MB

english, 2015

5

Novel 2,4-Disubstituted Pyrimidines as Potent, Selective, and Cell-Permeable Inhibitors of Neuronal Nitric Oxide Synthase

Mukherjee, Paramita, Li, Huiying, Sevrioukova, Irina, Chreifi, Georges, Martásek, Pavel, Roman, Linda J., Poulos, Thomas L., Silverman, Richard B.

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 3.70 MB

english, 2015

6

Antibacterial Drug Leads: DNA and Enzyme Multitargeting

Zhu, Wei, Wang, Yang, Li, Kai, Gao, Jian, Huang, Chun-Hsiang, Chen, Chun-Chi, Ko, Tzu-Ping, Zhang, Yonghui, Guo, Rey-Ting, Oldfield, Eric

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 1.34 MB

english, 2015

7

Metabotropic Glutamate Receptor 5 Negative Allosteric Modulators: Discovery of 2-Chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1 H -imidazol-4-ylethynyl]pyridine (Basimglurant, RO4917523), a Promising Novel Medicine for Psychiatric Diseases

Jaeschke, Georg, Kolczewski, Sabine, Spooren, Will, Vieira, Eric, Bitter-Stoll, Nadia, Boissin, Patrick, Borroni, Edilio, Büttelmann, Bernd, Ceccarelli, Simona, Clemann, Nicole, David, Beatrice, Funk,

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 1.97 MB

english, 2015

8

Fragment-Based Drug Discovery of 2-Thiazolidinones as BRD4 Inhibitors: 2. Structure-Based Optimization

Zhao, Lele, Wang, Yingqing, Cao, Danyan, Chen, Tiantian, Wang, Qi, Li, Yanlian, Xu, Yechun, Zhang, Naixia, Wang, Xin, Chen, Danqi, Chen, Lin, Chen, Yue-Lei, Xia, Guangxin, Shi, Zhe, Liu, Yu-Chih, Lin,

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 972 KB

english, 2015

9

Synthesis and Evaluation of Series of Diazine-Bridged Dinuclear Platinum(II) Complexes through in Vitro Toxicity and Molecular Modeling: Correlation between Structure and Activity of Pt(II) Complexes

Senerovic, Lidija, Zivkovic, Marija D., Veselinovic, Aleksandar, Pavic, Aleksandar, Djuran, Milos I., Rajkovic, Snezana, Nikodinovic-Runic, Jasmina

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 4.43 MB

english, 2015

10

Discovery of 1 H -Pyrazol-3(2 H )-ones as Potent and Selective Inhibitors of Protein Kinase R-like Endoplasmic Reticulum Kinase (PERK)

Smith, Adrian L., Andrews, Kristin L., Beckmann, Holger, Bellon, Steven F., Beltran, Pedro J., Booker, Shon, Chen, Hao, Chung, Young-Ah, D’Angelo, Noel D., Dao, Jennifer, Dellamaggiore, Kenneth R., Ja

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 4.42 MB

english, 2015

11

Function-Oriented Development of CXCR4 Antagonists as Selective Human Immunodeficiency Virus (HIV)-1 Entry Inhibitors

Wu, Chien-Huang, Wang, Chuan-Jen, Chang, Chun-Ping, Cheng, Yung-Chi, Song, Jen-Shin, Jan, Jiing-Jyh, Chou, Ming-Chen, Ke, Yi-Yu, Ma, Jing, Wong, Ying-Chieh, Hsieh, Tsung-Chih, Tien, Yun-Chen, Gullen,

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 7.48 MB

english, 2015

12

Computational Methods for Medicinal Chemistry

Bajorath, Jürgen, Jiang, Hualiang, Shoichet, Brian K., Walters, W. Patrick

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 117 KB

english, 2015

13

Promiscuous 2-Aminothiazoles (PrATs): A Frequent Hitting Scaffold

Devine, Shane M., Mulcair, Mark D., Debono, Cael O., Leung, Eleanor W. W., Nissink, J. Willem M., Lim, San Sui, Chandrashekaran, Indu R., Vazirani, Mansha, Mohanty, Biswaranjan, Simpson, Jamie S., Bae

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 1.24 MB

english, 2015

14

Design, Synthesis, and Biological Evaluation of Tetrazole Analogs of Cl-Amidine as Protein Arginine Deiminase Inhibitors

Subramanian, Venkataraman, Knight, Jason S., Parelkar, Sangram, Anguish, Lynne, Coonrod, Scott A., Kaplan, Mariana J., Thompson, Paul R.

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 942 KB

english, 2015

15

Novel 3-Nitrotriazole-Based Amides and Carbinols as Bifunctional Antichagasic Agents

Papadopoulou, Maria V., Bloomer, William D., Lepesheva, Galina I., Rosenzweig, Howard S., Kaiser, Marcel, Aguilera-Venegas, Benjamín, Wilkinson, Shane R., Chatelain, Eric, Ioset, Jean-Robert

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 1.38 MB

english, 2015

16

Design, Synthesis, and Biological Evaluation of Sulfonyl Acrylonitriles as Novel Inhibitors of Cancer Metastasis and Spread

Shen, Yi, Zificsak, Craig A., Shea, Jill E., Lao, Xuegang, Bollt, Oana, Li, Xiufen, Lisko, Joseph G., Theroff, Jay P., Scaife, Courtney L., Ator, Mark A., Ruggeri, Bruce A., Dorsey, Bruce D., Kuwada,

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 928 KB

english, 2015

17

Design, Synthesis, and Biological Evaluation of Combretabenzodiazepines: A Novel Class of Anti-Tubulin Agents

Galli, Ubaldina, Travelli, Cristina, Aprile, Silvio, Arrigoni, Elena, Torretta, Simone, Grosa, Giorgio, Massarotti, Alberto, Sorba, Giovanni, Canonico, Pier Luigi, Genazzani, Armando A., Tron, Gian Ce

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 2.29 MB

english, 2015

18

Identification of the Minimum Peptide from Mouse Myostatin Prodomain for Human Myostatin Inhibition

Takayama, Kentaro, Noguchi, Yuri, Aoki, Shin, Takayama, Shota, Yoshida, Momoko, Asari, Tomo, Yakushiji, Fumika, Nishimatsu, Shin-ichiro, Ohsawa, Yutaka, Itoh, Fumiko, Negishi, Yoichi, Sunada, Yoshihid

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 743 KB

english, 2015

19

Design, Synthesis, X-ray Crystallographic Analysis, and Biological Evaluation of Thiazole Derivatives as Potent and Selective Inhibitors of Human Dihydroorotate Dehydrogenase

Zhu, Junsheng, Han, Le, Diao, Yanyan, Ren, Xiaoli, Xu, Minghao, Xu, Liuxin, Li, Shiliang, Li, Qiang, Dong, Dong, Huang, Jin, Liu, Xiaofeng, Zhao, Zhenjiang, Wang, Rui, Zhu, Lili, Xu, Yufang, Qian, Xuh

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 1.02 MB

english, 2015

20

Development of a Series of Aryl Pyrimidine Kynurenine Monooxygenase Inhibitors as Potential Therapeutic Agents for the Treatment of Huntington’s Disease

Toledo-Sherman, Leticia M., Prime, Michael E., Mrzljak, Ladislav, Beconi, Maria G., Beresford, Alan, Brookfield, Frederick A., Brown, Christopher J., Cardaun, Isabell, Courtney, Stephen M., Dijkman, U

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 3.61 MB

english, 2015

21

Design, Synthesis, and Characterization of Fatty Acid Derivatives of a Dimeric Peptide-Based Postsynaptic Density-95 (PSD-95) Inhibitor

Nissen, Klaus B., Andersen, Julie J., Haugaard-Kedström, Linda M., Bach, Anders, Strømgaard, Kristian

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 320 KB

english, 2015

22

Synthesis and Evaluation of 4-Halogeno- N -[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]- N -[ 11 C]methylbenzamide for Imaging of Metabotropic Glutamate 1 Receptor in Melanoma

Fujinaga, Masayuki, Xie, Lin, Yamasaki, Tomoteru, Yui, Joji, Shimoda, Yoko, Hatori, Akiko, Kumata, Katsushi, Zhang, Yiding, Nengaki, Nobuki, Kawamura, Kazunori, Zhang, Ming-Rong

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 2.39 MB

english, 2015

23

Discovery of Potent Heterodimeric Antagonists of Inhibitor of Apoptosis Proteins (IAPs) with Sustained Antitumor Activity

Perez, Heidi L., Chaudhry, Charu, Emanuel, Stuart L., Fanslau, Caroline, Fargnoli, Joseph, Gan, Jinping, Kim, Kyoung S., Lei, Ming, Naglich, Joseph G., Traeger, Sarah C., Vuppugalla, Ragini, Wei, Donn

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 462 KB

english, 2015

24

Oleanane Triterpenes from the Flowers of Camellia japonica Inhibit Porcine Epidemic Diarrhea Virus (PEDV) Replication

Yang, Jun-Li, Ha, Thi-Kim-Quy, Dhodary, Basanta, Pyo, Euisun, Nguyen, Ngoc Hieu, Cho, Hyomoon, Kim, Eunhee, Oh, Won Keun

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 3.55 MB

english, 2015

25

Dual Antitumor and Antiangiogenic Activity of Organoplatinum(II) Complexes

Zamora, Ana, Pérez, Sergio A., Rodríguez, Venancio, Janiak, Christoph, Yellol, Gorakh S., Ruiz, José

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 9.56 MB

english, 2015

26

Carbonic Anhydrase Inhibitors with Dual-Tail Moieties To Match the Hydrophobic and Hydrophilic Halves of the Carbonic Anhydrase Active Site

Tanpure, Rajendra P., Ren, Bin, Peat, Thomas S., Bornaghi, Laurent F., Vullo, Daniela, Supuran, Claudiu T., Poulsen, Sally-Ann

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 1.17 MB

english, 2015

27

Exploration of Cyanine Compounds as Selective Inhibitors of Protein Arginine Methyltransferases: Synthesis and Biological Evaluation

Hu, Hao, Owens, Eric A., Su, Hairui, Yan, Leilei, Levitz, Andrew, Zhao, Xinyang, Henary, Maged, Zheng, Yujun George

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 5.44 MB

english, 2015

28

Simple Method Provides Resolution of Albumin, Lipoprotein, Free Fraction, and Chylomicron To Enhance the Utility of Protein Binding Assays

Brockman, Adam H., Oller, Haley R., Moreau, Benoît, Kriksciukaite, Kristina, Bilodeau, Mark T.

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 1.33 MB

english, 2015

29

2-(2-Oxo-morpholin-3-yl)-acetamide Derivatives as Broad-Spectrum Antifungal Agents

Bardiot, Dorothée, Thevissen, Karin, De Brucker, Katrijn, Peeters, Annelies, Cos, Paul, Taborda, Carlos P., McNaughton, Michael, Maes, Louis, Chaltin, Patrick, Cammue, Bruno P. A., Marchand, Arnaud

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 800 KB

english, 2015

30

Novel 5-Substituted Pyrrolo[2,3- d ]pyrimidines as Dual Inhibitors of Glycinamide Ribonucleotide Formyltransferase and 5-Aminoimidazole-4-carboxamide Ribonucleotide Formyltransferase and as Potential Antitumor Agents

Wang, Yiqiang, Mitchell-Ryan, Shermaine, Raghavan, Sudhir, George, Christina, Orr, Steven, Hou, Zhanjun, Matherly, Larry H., Gangjee, Aleem

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 1.23 MB

english, 2015

31

SAR-Guided Development and Characterization of a Potent Antitumor Compound toward B-Cell Neoplasms with No Detectable Cytotoxicity toward Healthy Cells

Brunhofer-Bolzer, Gerda, Le, Trang, Dyckmanns, Nils, Knaus, Hanna A., Pausz, Clemens, Freund, Patricia, Jäger, Ulrich, Erker, Thomas, Vanura, Katrina

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 1.39 MB

english, 2015

32

Structure–Activity Relationship for the Oxadiazole Class of Antibiotics

Spink, Edward, Ding, Derong, Peng, Zhihong, Boudreau, Marc A., Leemans, Erika, Lastochkin, Elena, Song, Wei, Lichtenwalter, Katerina, O’Daniel, Peter I., Testero, Sebastian A., Pi, Hualiang, Schroeder

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 2.16 MB

english, 2015

33

Proof of Concept Study for Designed Multiple Ligands Targeting the Dopamine D 2 , Serotonin 5-HT 2A , and Muscarinic M 1 Acetylcholine Receptors

Szabo, Monika, Lim, Herman D., Klein Herenbrink, Carmen, Christopoulos, Arthur, Lane, J. Robert, Capuano, Ben

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 595 KB

english, 2015

34

Novel Arylalkenylpropargylamines as Neuroprotective, Potent, and Selective Monoamine Oxidase B Inhibitors for the Treatment of Parkinson’s Disease

Huleatt, Paul B., Khoo, Mui Ling, Chua, Yi Yuan, Tan, Tiong Wei, Liew, Rou Shen, Balogh, Balázs, Deme, Ruth, Gölöncsér, Flóra, Magyar, Kalman, Sheela, David P., Ho, Han Kiat, Sperlágh, Beáta, Mátyus,

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 3.78 MB

english, 2015

35

3,4-Diaminobenzoic Acid Derivatives as Inhibitors of the Oxytocinase Subfamily of M1 Aminopeptidases with Immune-Regulating Properties

Papakyriakou, Athanasios, Zervoudi, Efthalia, Tsoukalidou, Sofia, Mauvais, Francois-Xavier, Sfyroera, Georgia, Mastellos, Dimitrios C., van Endert, Peter, Theodorakis, Emmanuel A., Vourloumis, Dionisi

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 5.89 MB

english, 2015

36

A Series of Novel Terpyridine-Skeleton Molecule Derivants Inhibit Tumor Growth and Metastasis by Targeting Topoisomerases

Kwon, Han-Byeol, Park, Chanmi, Jeon, Kyung-Hwa, Lee, Eunyoung, Park, So-Eun, Jun, Kyu-Yeon, Kadayat, Tara Man, Thapa, Pritam, Karki, Radha, Na, Younghwa, Park, Mi Sun, Rho, Seung Bae, Lee, Eung-Seok,

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 2.79 MB

english, 2015

37

Design and Synthesis of Potent and Multifunctional Aldose Reductase Inhibitors Based on Quinoxalinones

Qin, Xiangyu, Hao, Xin, Han, Hui, Zhu, Shaojuan, Yang, Yanchun, Wu, Bobin, Hussain, Saghir, Parveen, Shagufta, Jing, Chaojun, Ma, Bing, Zhu, Changjin

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 2.56 MB

english, 2015

38

Synthetic Peptides Reproducing Tissue Transglutaminase–Gliadin Complex Neo-epitopes as Probes for Antibody Detection in Celiac Disease Patients’ Sera

Di Pisa, Margherita, Pascarella, Simona, Scrima, Mario, Sabatino, Giuseppina, Real-Fernández, Feliciana, Chelli, Mario, Renzi, Daniela, Calabrò, Antonio, D’Ursi, Anna Maria, Papini, Anna Maria, Rovero

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 2.08 MB

english, 2015

39

Cell-Permeable Inhibitors of Neuronal Nitric Oxide Synthase Open New Prospects for the Treatment of Neurological Disorders

Annedi, Subhash C.

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 320 KB

english, 2015

40

Highly Selective Salicylketoxime-Based Estrogen Receptor β Agonists Display Antiproliferative Activities in a Glioma Model

Paterni, Ilaria, Bertini, Simone, Granchi, Carlotta, Tuccinardi, Tiziano, Macchia, Marco, Martinelli, Adriano, Caligiuri, Isabella, Toffoli, Giuseppe, Rizzolio, Flavio, Carlson, Kathryn E., Katzenelle

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 2.28 MB

english, 2015

41

Synthesis and Biological Evaluation of Second-Generation Tropanol-Based Androgen Receptor Modulators

Sundén, Henrik, Holland, Mareike C., Poutiainen, Pekka K., Jääskeläinen, Tiina, Pulkkinen, Juha T., Palvimo, Jorma J., Olsson, Roger

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 1.24 MB

english, 2015

42

A High-Throughput Screen Reveals New Small-Molecule Activators and Inhibitors of Pantothenate Kinases

Sharma, Lalit Kumar, Leonardi, Roberta, Lin, Wenwei, Boyd, Vincent A., Goktug, Asli, Shelat, Anang A., Chen, Taosheng, Jackowski, Suzanne, Rock, Charles O.

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 1.34 MB

english, 2015

43

Pachymodulin, a New Functional Formyl Peptide Receptor 2 Peptidic Ligand Isolated from Frog Skin Has Janus-like Immunomodulatory Capacities

Lacombe, Claire, Piesse, Christophe, Sagan, Sandrine, Combadière, Christophe, Rosenstein, Yvonne, Auvynet, Constance

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 3.49 MB

english, 2015

44

Glycosylated Enfuvirtide: A Long-Lasting Glycopeptide with Potent Anti-HIV Activity

Cheng, Shuihong, Chang, Xuesong, Wang, Yan, Gao, George F., Shao, Yiming, Ma, Liying, Li, Xuebing

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 1.37 MB

english, 2015

45

Development of Potent Inhibitors of Pyocyanin Production in Pseudomonas aeruginosa

Miller, Laura C., O’Loughlin, Colleen T., Zhang, Zinan, Siryaporn, Albert, Silpe, Justin E., Bassler, Bonnie L., Semmelhack, Martin F.

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 846 KB

english, 2015

46

Discovery of Small Molecule Inhibitors to Krüppel-like Factor 10 (KLF10): Implications for Modulation of T Regulatory Cell Differentiation

Khedkar, Santosh A., Sun, Xinghui, Rigby, Alan C., Feinberg, Mark W.

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 1.58 MB

english, 2015