Volume 56; Issue 22

Journal of Medicinal Chemistry

Volume 56; Issue 22

1

A Medicinal Chemistry Perspective for Targeting Histone H3 Lysine-79 Methyltransferase DOT1L

Anglin, Justin L., Song, Yongcheng

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 579 KB

english, 2013

2

Polypharmacology – Foe or Friend?

Peters, Jens-Uwe

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 1.72 MB

english, 2013

3

A Structure–Activity Analysis of Biased Agonism at the Dopamine D2 Receptor

Shonberg, Jeremy, Herenbrink, Carmen Klein, López, Laura, Christopoulos, Arthur, Scammells, Peter J., Capuano, Ben, Lane, J. Robert

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 1.73 MB

english, 2013

4

Conformationally Constrained ortho- Anilino Diaryl Ureas: Discovery of 1-(2-(1′-Neopentylspiro[indoline-3,4′-piperidine]-1-yl)phenyl)-3-(4-(trifluoromethoxy)phenyl)urea, a Potent, Selective, and Bioavailable P2Y 1 Antagonist

Qiao, Jennifer X., Wang, Tammy C., Ruel, Réjean, Thibeault, Carl, L’Heureux, Alexandre, Schumacher, William A., Spronk, Steven A., Hiebert, Sheldon, Bouthillier, Gilles, Lloyd, John, Pi, Zulan, Schnur

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 1004 KB

english, 2013

5

Structure–Activity Relationships and Molecular Modeling of Sphingosine Kinase Inhibitors

Baek, Dong Jae, MacRitchie, Neil, Anthony, Nahoum G., Mackay, Simon P., Pyne, Susan, Pyne, Nigel J., Bittman, Robert

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 2.68 MB

english, 2013

6

Discovery of the First M 5 -Selective and CNS Penetrant Negative Allosteric Modulator (NAM) of a Muscarinic Acetylcholine Receptor: ( S )-9b-(4-Chlorophenyl)-1-(3,4-difluorobenzoyl)-2,3-dihydro-1 H -imidazo[2,1- a ]isoindol-5(9b H )-one (ML375)

Gentry, Patrick R., Kokubo, Masaya, Bridges, Thomas M., Kett, Nathan R., Harp, Joel M., Cho, Hyekyung P., Smith, Emery, Chase, Peter, Hodder, Peter S., Niswender, Colleen M., Daniels, J. Scott, Conn,

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 716 KB

english, 2013

7

Concise Synthesis and Biological Evaluation of 2-Aroyl-5-Amino Benzo[ b ]thiophene Derivatives As a Novel Class of Potent Antimitotic Agents

Romagnoli, Romeo, Baraldi, Pier Giovanni, Lopez-Cara, Carlota, Preti, Delia, Aghazadeh Tabrizi, Mojgan, Balzarini, Jan, Bassetto, Marcella, Brancale, Andrea, Fu, Xian-Hua, Gao, Yang, Li, Jun, Zhang, S

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 2.64 MB

english, 2013

8

3-Azatetracyclo[5.2.1.1 5,8 .0 1,5 ]undecane Derivatives: From Wild-Type Inhibitors of the M2 Ion Channel of Influenza A Virus to Derivatives with Potent Activity against the V27A Mutant

Rey-Carrizo, Matias, Torres, Eva, Ma, Chunlong, Barniol-Xicota, Marta, Wang, Jun, Wu, Yibing, Naesens, Lieve, DeGrado, William F., Lamb, Robert A., Pinto, Lawrence H., Vázquez, Santiago

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 458 KB

english, 2013

9

Development of a Mucin4-Targeting SPIO Contrast Agent for Effective Detection of Pancreatic Tumor Cells in Vitro and in Vivo

Wu, Shou-Cheng, Chen, Yu-Jen, Lin, Yi-Jan, Wu, Tung-Ho, Wang, Yun-Ming

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 4.93 MB

english, 2013

10

Discovery and Characterization of a Novel Dihydroisoxazole Class of α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) Receptor Potentiators

Patel, Nandini C., Schwarz, Jacob, Hou, Xinjun J., Hoover, Dennis J., Xie, Longfei, Fliri, Anton J., Gallaschun, Randall J., Lazzaro, John T., Bryce, Dianne K., Hoffmann, William E., Hanks, Ashley N.,

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 1.21 MB

english, 2013

11

A Selective Mitochondrial-Targeted Chlorambucil with Remarkable Cytotoxicity in Breast and Pancreatic Cancers

Millard, Melissa, Gallagher, John D., Olenyuk, Bogdan Z., Neamati, Nouri

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 1.42 MB

english, 2013

12

Bifunctional PEGylated Exenatide-Amylinomimetic Hybrids to Treat Metabolic Disorders: An Example of Long-Acting Dual Hormonal Therapeutics

Sun, Chengzao, Trevaskis, James L., Jodka, Carolyn M., Neravetla, Swetha, Griffin, Pete, Xu, Kui, Wang, Yan, Parkes, David G., Forood, Bruce, Ghosh, Soumitra S.

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 2.66 MB

english, 2013

13

Correction to 3-Thiomorpholin-8-oxo-8 H -acenaphtho[1,2- b ]pyrrole-9-carbonitrile (S1) Based Molecules as Potent, Dual Inhibitors of B-Cell Lymphoma 2 (Bcl-2) and Myeloid Cell Leukemia Sequence 1 (Mcl-1): Structure-Based Design and Structure–Activity Relationship Studies

Song, Ting, Chen, Qingbin, Li, Xiangqian, Chai, Gaobo, Zhang, Zhichao

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 1.86 MB

english, 2013

14

Aminothiazole-Featured Pirinixic Acid Derivatives As Dual 5-Lipoxygenase and Microsomal Prostaglandin E 2 Synthase-1 Inhibitors with Improved Potency and Efficiency in Vivo

Hanke, Thomas, Dehm, Friederike, Liening, Stefanie, Popella, Sven-Desiderius, Maczewsky, Jonas, Pillong, Max, Kunze, Jens, Weinigel, Christina, Barz, Dagmar, Kaiser, Astrid, Wurglics, Mario, Lämmerhof

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 2.33 MB

english, 2013

15

Correction to Discovery of (2 R )-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1 H -indol-1-yl}phenoxy)butanoic Acid (MK-0533): A Novel Selective Peroxisome Proliferator-Activated Receptor γ Modulator for the Treatment of Type 2 Diabetes Mellitus with a Reduced Potential to Increase Plasma and Extracellular Fluid Volume

Acton, John J., Akiyama, Taro E., Chang, Ching H., Colwell, Lawrence, Debenham, Sheryl, Doebber, Thomas, Einstein, Monica, Liu, Kun, McCann, Margaret E., Moller, David E., Muise, Eric S., Tan, Yejun,

Journal:

Journal of Medicinal Chemistry

Année:

2013

Fichier:

PDF, 112 KB

2013

16

2′-Deoxyuridine 5′-Monophosphate Substrate Displacement in Thymidylate Synthase through 6-Hydroxy-2 H -naphtho[1,8- bc ]furan-2-one Derivatives

Ferrari, Stefania, Calò, Samuele, Leone, Rosalida, Luciani, Rosaria, Costantino, Luca, Sammak, Susan, Di Pisa, Flavio, Pozzi, Cecilia, Mangani, Stefano, Costi, M. Paola

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 755 KB

english, 2013

17

Optimization of Novel Indole-2-carboxamide Inhibitors of Neurotropic Alphavirus Replication

Sindac, Janice A., Barraza, Scott J., Dobry, Craig J., Xiang, Jianming, Blakely, Pennelope K., Irani, David N., Keep, Richard F., Miller, David J., Larsen, Scott D.

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 1.09 MB

english, 2013

18

Synthesis and Biological Evaluation of Aryloxazole Derivatives as Antimitotic and Vascular-Disrupting Agents for Cancer Therapy

Choi, Min Jeong, No, Eun Sun, Thorat, Dhanaji Achyutrao, Jang, Jae Wan, Yang, Hakkyun, Lee, Jaeick, Choo, Hyunah, Kim, Soo Jin, Lee, Chang Sik, Ko, Soo Young, Lee, Jiyoun, Nam, GhilSoo, Pae, Ae Nim

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 2.92 MB

english, 2013

19

Rapid Identification of Ligand-Binding Sites by Using an Assignment-Free NMR Approach

Kodama, Yuya, Takeuchi, Koh, Shimba, Nobuhisa, Ishikawa, Kohki, Suzuki, Ei-ichiro, Shimada, Ichio, Takahashi, Hideo

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 2.44 MB

english, 2013

20

Structure–Activity Relationship of Imidazopyridinium Analogues as Antagonists of Neuropeptide S Receptor

Patnaik, Samarjit, Marugan, Juan J., Liu, Ke, Zheng, Wei, Southall, Noel, Dehdashti, Seameen J., Thorsell, Annika, Heilig, Markus, Bell, Lauren, Zook, Michelle, Eskay, Bob, Brimacombe, Kyle R., Austin

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 1.39 MB

english, 2013

21

Design and Synthesis of P1–P3 Macrocyclic Tertiary-Alcohol-Comprising HIV-1 Protease Inhibitors

Joshi, Advait, Véron, Jean-Baptiste, Unge, Johan, Rosenquist, Åsa, Wallberg, Hans, Samuelsson, Bertil, Hallberg, Anders, Larhed, Mats

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 2.54 MB

english, 2013

22

Synthesis and Evaluation of a 18 F-Labeled Diarylpyrazole Glycoconjugate for the Imaging of NTS1-Positive Tumors

Lang, Christopher, Maschauer, Simone, Hübner, Harald, Gmeiner, Peter, Prante, Olaf

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 1.44 MB

english, 2013

23

Discovery of a Potent Inhibitor of Replication Protein A Protein–Protein Interactions Using a Fragment-Linking Approach

Frank, Andreas O., Feldkamp, Michael D., Kennedy, J. Phillip, Waterson, Alex G., Pelz, Nicholas F., Patrone, James D., Vangamudi, Bhavatarini, Camper, DeMarco V., Rossanese, Olivia W., Chazin, Walter

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 3.33 MB

english, 2013

24

Aurora Isoform Selectivity: Design and Synthesis of Imidazo[4,5- b ]pyridine Derivatives as Highly Selective Inhibitors of Aurora-A Kinase in Cells

Bavetsias, Vassilios, Faisal, Amir, Crumpler, Simon, Brown, Nathan, Kosmopoulou, Magda, Joshi, Amar, Atrash, Butrus, Pérez-Fuertes, Yolanda, Schmitt, Jessica A., Boxall, Katherine J., Burke, Rosemary,

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 4.51 MB

english, 2013

25

Design, Synthesis, and Biological Evaluation of 14-Heteroaromatic-Substituted Naltrexone Derivatives: Pharmacological Profile Switch from Mu Opioid Receptor Selectivity to Mu/Kappa Opioid Receptor Dual Selectivity

Yuan, Yunyun, Zaidi, Saheem A., Elbegdorj, Orgil, Aschenbach, Lindsey C. K., Li, Guo, Stevens, David L., Scoggins, Krista L., Dewey, William L., Selley, Dana E., Zhang, Yan

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 2.95 MB

english, 2013

26

Nicotinamide Phosphoribosyltransferase Inhibitors, Design, Preparation, and Structure–Activity Relationship

Christensen, Mette K., Erichsen, Kamille D., Olesen, Uffe H., Tjørnelund, Jette, Fristrup, Peter, Thougaard, Annemette, Nielsen, Søren Jensby, Sehested, Maxwell, Jensen, Peter B., Loza, Einars, Kalvin

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 3.76 MB

english, 2013

27

Synthesis and Evaluation of Multi-Target-Directed Ligands against Alzheimer’s Disease Based on the Fusion of Donepezil and Ebselen

Luo, Zonghua, Sheng, Jianfei, Sun, Yang, Lu, Chuanjun, Yan, Jun, Liu, Anqiu, Luo, Hai-bin, Huang, Ling, Li, Xingshu

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 1.15 MB

english, 2013

28

Structure-Guided Design of Potent Diazobenzene Inhibitors for the BET Bromodomains

Zhang, Guangtao, Plotnikov, Alexander N., Rusinova, Elena, Shen, Tong, Morohashi, Keita, Joshua, Jennifer, Zeng, Lei, Mujtaba, Shiraz, Ohlmeyer, Michael, Zhou, Ming-Ming

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 3.61 MB

english, 2013

29

Novel, Broad-Spectrum Anticonvulsants Containing a Sulfamide Group: Pharmacological Properties of ( S )- N -[(6-Chloro-2,3-dihydrobenzo[1,4]dioxin-2-yl)methyl]sulfamide (JNJ-26489112)

McComsey, David F., Smith-Swintosky, Virginia L., Parker, Michael H., Brenneman, Douglas E., Malatynska, Ewa, White, H. Steve, Klein, Brian D., Wilcox, Karen S., Milewski, Michael E., Herb, Mark, Finl

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 582 KB

english, 2013

30

Modulation of the Fibrillogenesis Inhibition Properties of Two Transthyretin Ligands by Halogenation

Cotrina, Ellen Y., Pinto, Marta, Bosch, Lluís, Vilà, Marta, Blasi, Daniel, Quintana, Jordi, Centeno, Nuria B., Arsequell, Gemma, Planas, Antoni, Valencia, Gregorio

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 2.30 MB

english, 2013

31

Naturally Occurring Antimicrobial Peptide OH-CATH30 Selectively Regulates the Innate Immune Response To Protect against Sepsis

Li, Sheng-An, Xiang, Yang, Wang, Yan-Jie, Liu, Jie, Lee, Wen-Hui, Zhang, Yun

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 4.01 MB

english, 2013

32

Structure–Activity Relationship Study of Permethyl Ningalin B Analogues as P-Glycoprotein Chemosensitizers

Bin, Jin Wen, Wong, Iris L. K., Hu, Xuesen, Yu, Zhang Xiao, Xing, Li Fu, Jiang, Tao, Chow, Larry M. C., Biao, Wan Sheng

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 1.11 MB

english, 2013

33

In Vitro Metabolic Profile and in Vivo Antischistosomal Activity Studies of (η 6 -Praziquantel)Cr(CO) 3 Derivatives

Patra, Malay, Ingram, Katrin, Leonidova, Anna, Pierroz, Vanessa, Ferrari, Stefano, Robertson, Murray N., Todd, Matthew H., Keiser, Jennifer, Gasser, Gilles

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 536 KB

english, 2013

34

In Vitro and in Vivo Antileishmanial and Trypanocidal Studies of New N -Benzene- and N -Naphthalenesulfonamide Derivatives

Galiana-Roselló, Cristina, Bilbao-Ramos, Pablo, Dea-Ayuela, M. Auxiliadora, Rolón, Miriam, Vega, Celeste, Bolás-Fernández, Francisco, García-España, Enrique, Alfonso, Jorge, Coronel, Cathia, González-

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 2.02 MB

english, 2013

35

Synthesis and Evaluation in Monkey of [ 18 F]4-Fluoro- N -methyl- N -(4-(6-(methylamino)pyrimidin-4-yl)thiazol-2-yl)benzamide ([ 18 F]FIMX): A Promising Radioligand for PET Imaging of Brain Metabotropic Glutamate Receptor 1 (mGluR1)

Xu, Rong, Zanotti-Fregonara, Paolo, Zoghbi, Sami S., Gladding, Robert L., Woock, Alicia E., Innis, Robert B., Pike, Victor W

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 1.42 MB

english, 2013