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Volume 58; Issue 8

Journal of Medicinal Chemistry

Volume 58; Issue 8

1

Small Molecule Discoidin Domain Receptor Kinase Inhibitors and Potential Medical Applications

Li, Yupeng, Lu, Xiaoyun, Ren, Xiaomei, Ding, Ke

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 3.17 MB

english, 2015

2

Antimalarial Activity of 4-Amidinoquinoline and 10-Amidinobenzonaphthyridine Derivatives

Korotchenko, Vasiliy, Sathunuru, Ramadas, Gerena, Lucia, Caridha, Diana, Li, Qigui, Kreishman-Deitrick, Mara, Smith, Philip L., Lin, Ai J.

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 967 KB

english, 2015

3

(Dis)similar Analogues of Riboswitch Metabolites as Antibacterial Lead Compounds

Matzner, Daniel, Mayer, Günter

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 1.93 MB

english, 2015

4

Discovery of Intestinal Targeted TGR5 Agonists for the Treatment of Type 2 Diabetes

Duan, Hongliang, Ning, Mengmeng, Zou, Qingan, Ye, Yangliang, Feng, Ying, Zhang, Lina, Leng, Ying, Shen, Jianhua

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 997 KB

english, 2015

5

Niraparib: A Poly(ADP-ribose) Polymerase (PARP) Inhibitor for the Treatment of Tumors with Defective Homologous Recombination

Jones, Philip, Wilcoxen, Keith, Rowley, Michael, Toniatti, Carlo

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 2.41 MB

english, 2015

6

Neuroactive Steroids. 1. Positive Allosteric Modulators of the (γ-Aminobutyric Acid) A Receptor: Structure–Activity Relationships of Heterocyclic Substitution at C-21

Martinez Botella, Gabriel, Salituro, Francesco G., Harrison, Boyd L., Beresis, Richard T., Bai, Zhu, Shen, Kaisheng, Belfort, Gabriel M., Loya, Carlos M., Ackley, Michael A., Grossman, Scott J., Hoffm

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 555 KB

english, 2015

7

Modulating the Anticancer Activity of Ruthenium(II)–Arene Complexes

Clavel, Catherine M., Păunescu, Emilia, Nowak-Sliwinska, Patrycja, Griffioen, Arjan W., Scopelliti, Rosario, Dyson, Paul J.

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 1.11 MB

english, 2015

8

Hotspots in an Obligate Homodimeric Anticancer Target. Structural and Functional Effects of Interfacial Mutations in Human Thymidylate Synthase

Salo-Ahen, Outi M. H., Tochowicz, Anna, Pozzi, Cecilia, Cardinale, Daniela, Ferrari, Stefania, Boum, Yap, Mangani, Stefano, Stroud, Robert M., Saxena, Puneet, Myllykallio, Hannu, Costi, Maria Paola, P

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 1.40 MB

english, 2015

9

Discovery of Potent Inhibitors of Schistosoma mansoni NAD + Catabolizing Enzyme

Jacques, Sylvain A., Kuhn, Isabelle, Koniev, Oleksandr, Schuber, Francis, Lund, Frances E., Wagner, Alain, Muller-Steffner, Hélène, Kellenberger, Esther

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 664 KB

english, 2015

10

Design and Synthesis of New α-Naphthoflavones as Cytochrome P450 (CYP) 1B1 Inhibitors To Overcome Docetaxel-Resistance Associated with CYP1B1 Overexpression

Cui, Jiahua, Meng, Qingqing, Zhang, Xu, Cui, Qing, Zhou, Wen, Li, Shaoshun

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 1.13 MB

english, 2015

11

Selective Inhibitors of Cyclin G Associated Kinase (GAK) as Anti-Hepatitis C Agents

Kovackova, Sona, Chang, Lei, Bekerman, Elena, Neveu, Gregory, Barouch-Bentov, Rina, Chaikuad, Apirat, Heroven, Christina, Šála, Michal, De Jonghe, Steven, Knapp, Stefan, Einav, Shirit, Herdewijn, Piet

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 1.46 MB

english, 2015

12

Design and Synthesis of Antitumor Heck-Coupled Sclareol Analogues: Modulation of BH3 Family Members by SS-12 in Autophagy and Apoptotic Cell Death

Shakeel-u-Rehman,, Rah, Bilal, Lone, Shabir H., Rasool, Reyaz Ur, Farooq, Saleem, Nayak, Debasis, Chikan, Naveed Anjum, Chakraborty, Souneek, Behl, Akanksha, Mondhe, Dilip Manikaro, Goswami, Anindya,

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 1.35 MB

english, 2015

13

The Discovery of Orally Bioavailable Tyrosine Threonine Kinase (TTK) Inhibitors: 3-(4-(heterocyclyl)phenyl)-1 H -indazole-5-carboxamides as Anticancer Agents

Liu, Yong, Lang, Yunhui, Patel, Narendra Kumar, Ng, Grace, Laufer, Radoslaw, Li, Sze-Wan, Edwards, Louise, Forrest, Bryan, Sampson, Peter B., Feher, Miklos, Ban, Fuqiang, Awrey, Donald E., Beletskaya,

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 7.22 MB

english, 2015

14

Approved Drugs Containing Thiols as Inhibitors of Metallo-β-lactamases: Strategy To Combat Multidrug-Resistant Bacteria

Klingler, Franca-M., Wichelhaus, Thomas A., Frank, Denia, Cuesta-Bernal, Jenifer, El-Delik, Jasmin, Müller, H. Florian, Sjuts, Hanno, Göttig, Stephan, Koenigs, Arno, Pos, Klaas M., Pogoryelov, Denys,

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 499 KB

english, 2015

15

Discovery of Orally Available Runt-Related Transcription Factor 3 (RUNX3) Modulators for Anticancer Chemotherapy by Epigenetic Activation and Protein Stabilization

Yang, Jee Sun, Lee, Chulho, Cho, Misun, Kim, Hyuntae, Kim, Jae Hyun, Choi, Seonghwi, Oh, Soo Jin, Kang, Jong Soon, Jeong, Jin-Hyun, Kim, Hyun-Jung, Han, Gyoonhee

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 548 KB

english, 2015

16

Discovery, Synthesis, and Biological Evaluation of Thiazoloquin(az)olin(on)es as Potent CD38 Inhibitors

Haffner, Curt D., Becherer, J. David, Boros, Eric E., Cadilla, Rodolfo, Carpenter, Tiffany, Cowan, David, Deaton, David N., Guo, Yu, Harrington, Wallace, Henke, Brad R., Jeune, Michael R., Kaldor, Ist

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 3.13 MB

english, 2015

17

New Organochalcogen Multitarget Drug: Synthesis and Antioxidant and Antitumoral Activities of Chalcogenozidovudine Derivatives

de Souza, Diego, Mariano, Douglas O. C., Nedel, Fernanda, Schultze, Eduarda, Campos, Vinícius F., Seixas, Fabiana, da Silva, Rafael S., Munchen, Taiana S., Ilha, Vinicius, Dornelles, Luciano, Braga, A

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 5.22 MB

english, 2015

18

β- d -2′- C -Methyl-2,6-diaminopurine Ribonucleoside Phosphoramidates are Potent and Selective Inhibitors of Hepatitis C Virus (HCV) and Are Bioconverted Intracellularly to Bioactive 2,6-Diaminopurine and Guanosine 5′-Triphosphate Forms

Zhou, Longhu, Zhang, Hong-wang, Tao, Sijia, Bassit, Leda, Whitaker, Tony, McBrayer, Tamara R., Ehteshami, Maryam, Amiralaei, Sheida, Pradere, Ugo, Cho, Jong Hyun, Amblard, Franck, Bobeck, Drew, Detori

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 2.11 MB

english, 2015

19

Structure-Based Design of Potent and Selective Inhibitors of the Metabolic Kinase PFKFB3

Boyd, Scott, Brookfield, Joanna L., Critchlow, Susan E., Cumming, Iain A., Curtis, Nicola J., Debreczeni, Judit, Degorce, Sébastien L., Donald, Craig, Evans, Nicola J., Groombridge, Sam, Hopcroft, Phi

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 1.13 MB

english, 2015

20

Correction to α 2 -Adrenoceptor Antagonists: Synthesis, Pharmacological Evaluation, and Molecular Modeling Investigation of Pyridinoguanidine, Pyridino-2-aminoimidazoline and Their Derivatives

Kelly, Brendan, McMullan, Michela, Muguruza, Carolina, Ortega, Jorge E., Meana, J. Javier, Callado, Luis F., Rozas, Isabel

Journal:

Journal of Medicinal Chemistry

Année:

2015

Fichier:

PDF, 114 KB

2015

21

Investigation of ( E )-3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators

Degorce, Sébastien L., Bailey, Andrew, Callis, Rowena, De Savi, Chris, Ducray, Richard, Lamont, Gillian, MacFaul, Philip, Maudet, Mickael, Martin, Scott, Morgentin, Rémy, Norman, Richard A., Peru, Aur

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 3.39 MB

english, 2015

22

Evaluation of 3-Ethyl-3-(phenylpiperazinylbutyl)oxindoles as PET Ligands for the Serotonin 5-HT 7 Receptor: Synthesis, Pharmacology, Radiolabeling, and in Vivo Brain Imaging in Pigs

Herth, Matthias M., Andersen, Valdemar L., Hansen, Hanne D., Stroth, Nikolas, Volk, Balázs, Lehel, Szabolcs, Dyssegaard, Agnete, Ettrup, Anders, Svenningsson, Per, Knudsen, Gitte M., Kristensen, Jespe

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 1.95 MB

english, 2015

23

Synthesis of β-Carboline-Based N -Heterocyclic Carbenes and Their Antiproliferative and Antimetastatic Activities against Human Breast Cancer Cells

Dighe, Shashikant U., Khan, Sajid, Soni, Isha, Jain, Preeti, Shukla, Samriddhi, Yadav, Rajeev, Sen, Pratik, Meeran, Syed M., Batra, Sanjay

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 1003 KB

english, 2015

24

Nicotinic Acid Adenine Dinucleotide Phosphate Analogues Substituted on the Nicotinic Acid and Adenine Ribosides. Effects on ReceptorMediated Ca 2+ Release

Trabbic, Christopher J., Zhang, Fan, Walseth, Timothy F., Slama, James T.

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 1.15 MB

english, 2015

25

Rational Design of Triazololipopeptides Analogs of Kisspeptin Inducing a Long-Lasting Increase of Gonadotropins

Beltramo, Massimiliano, Robert, Vincent, Galibert, Mathieu, Madinier, Jean-Baptiste, Marceau, Philippe, Dardente, Hugues, Decourt, Caroline, De Roux, Nicolas, Lomet, Didier, Delmas, Agnès F., Caraty,

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 2.09 MB

english, 2015

26

Correction to Imidazol-1-ylethylindazole Voltage-Gated Sodium Channel Ligands Are Neuroprotective during Optic Neuritis in a Mouse Model of Multiple Sclerosis

Browne, Lorcan, Lidster, Katie, Al-Izki, Sarah, Clutterbuck, Lisa, Posada, Cristina, Chan, A. W. Edith, Riddall, Dieter, Garthwaite, John, Baker, David, Selwood, David L.

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 169 KB

english, 2015

27

Synthesis and Evaluation of Fluorinated Fingolimod (FTY720) Analogues for Sphingosine-1-Phosphate Receptor Molecular Imaging by Positron Emission Tomography

Shaikh, Rizwan S., Schilson, Stefanie S., Wagner, Stefan, Hermann, Sven, Keul, Petra, Levkau, Bodo, Schäfers, Michael, Haufe, Günter

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 3.59 MB

english, 2015

28

Combinatorial Libraries As a Tool for the Discovery of Novel, Broad-Spectrum Antibacterial Agents Targeting the ESKAPE Pathogens

Fleeman, Renee, LaVoi, Travis M., Santos, Radleigh G., Morales, Angela, Nefzi, Adel, Welmaker, Gregory S., Medina-Franco, José L., Giulianotti, Marc A., Houghten, Richard A., Shaw, Lindsey N.

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 2.83 MB

english, 2015