Volume 56; Issue 14

Journal of Medicinal Chemistry

Volume 56; Issue 14

1

Discovery of Innovative Therapeutics: Today’s Realities and Tomorrow’s Vision. 1. Criticisms Faced by the Pharmaceutical Industry

Abou-Gharbia, Magid, Childers, Wayne E.

Journal:

Journal of Medicinal Chemistry

Year:

2013

Language:

english

File:

PDF, 1.93 MB

english, 2013

2

Inhibition of Rhodesain as a Novel Therapeutic Modality for Human African Trypanosomiasis

Ettari, Roberta, Tamborini, Lucia, Angelo, Ilenia C., Micale, Nicola, Pinto, Andrea, De Micheli, Carlo, Conti, Paola

Journal:

Journal of Medicinal Chemistry

Year:

2013

Language:

english

File:

PDF, 2.30 MB

english, 2013

3

Synthesis, Structure–Activity Relationships, and in Vivo Efficacy of the Novel Potent and Selective Anaplastic Lymphoma Kinase (ALK) Inhibitor 5-Chloro- N 2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)- N 4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) Currently in Phase 1 and Phase 2 Clinical Trials

Marsilje, Thomas H., Pei, Wei, Chen, Bei, Lu, Wenshuo, Uno, Tetsuo, Jin, Yunho, Jiang, Tao, Kim, Sungjoon, Li, Nanxin, Warmuth, Markus, Sarkisova, Yelena, Sun, Frank, Steffy, Auzon, Pferdekamper, Anne

Journal:

Journal of Medicinal Chemistry

Year:

2013

Language:

english

File:

PDF, 1.22 MB

english, 2013

4

(Biphenyl-4-yl)methylammonium Chlorides: Potent Anticonvulsants That Modulate Na + Currents

Lee, Hyosung, Park, Ki Duk, Yang, Xiao-Fang, Dustrude, Erik T., Wilson, Sarah M., Khanna, Rajesh, Kohn, Harold

Journal:

Journal of Medicinal Chemistry

Year:

2013

Language:

english

File:

PDF, 1.64 MB

english, 2013

5

Accurate Models for P-gp Drug Recognition Induced from a Cancer Cell Line Cytotoxicity Screen

Levatić, Jurica, Ćurak, Jasna, Kralj, Marijeta, Šmuc, Tomislav, Osmak, Maja, Supek, Fran

Journal:

Journal of Medicinal Chemistry

Year:

2013

Language:

english

File:

PDF, 2.46 MB

english, 2013

6

Histone Deacetylase Inhibitors Equipped with Estrogen Receptor Modulation Activity

Gryder, Berkley E., Rood, Michael K., Johnson, Kenyetta A., Patil, Vishal, Raftery, Eric D., Yao, Li-Pan D., Rice, Marcie, Azizi, Bahareh, Doyle, Donald F., Oyelere, Adegboyega K.

Journal:

Journal of Medicinal Chemistry

Year:

2013

Language:

english

File:

PDF, 1.95 MB

english, 2013

7

Potential Anticancer Heterometallic Fe–Au and Fe–Pd Agents: Initial Mechanistic Insights

Lease, Nicholas, Vasilevski, Vadim, Carreira, Monica, de Almeida, Andreia, Sanaú, Mercedes, Hirva, Pipsa, Casini, Angela, Contel, María

Journal:

Journal of Medicinal Chemistry

Year:

2013

Language:

english

File:

PDF, 740 KB

english, 2013

8

Selective Cannabinoid Receptor Type 2 (CB2) Agonists: Optimization of a Series of Purines Leading to the Identification of a Clinical Candidate for the Treatment of Osteoarthritic Pain

Hollinshead, Sean P., Tidwell, Michael W., Palmer, John, Guidetti, Rossella, Sanderson, Adam, Johnson, Michael P., Chambers, Mark G., Oskins, Jennifer, Stratford, Robert, Astles, Peter C.

Journal:

Journal of Medicinal Chemistry

Year:

2013

Language:

english

File:

PDF, 739 KB

english, 2013

9

Mahanine, A DNA Minor Groove Binding Agent Exerts Cellular Cytotoxicity with Involvement of C-7-OH and −NH Functional Groups

Samanta, Suman K., Dutta, Devawati, Roy, Sarita, Bhattacharya, Kaushik, Sarkar, Sayantani, Dasgupta, Anjan K., Pal, Bikas C., Mandal, Chhabinath, Mandal, Chitra

Journal:

Journal of Medicinal Chemistry

Year:

2013

Language:

english

File:

PDF, 4.61 MB

english, 2013

10

Rational Design of Sulfonated A 3 Adenosine Receptor-Selective Nucleosides as Pharmacological Tools To Study Chronic Neuropathic Pain

Paoletta, Silvia, Tosh, Dilip K., Finley, Amanda, Gizewski, Elizabeth T., Moss, Steven M., Gao, Zhan-Guo, Auchampach, John A., Salvemini, Daniela, Jacobson, Kenneth A.

Journal:

Journal of Medicinal Chemistry

Year:

2013

Language:

english

File:

PDF, 1.84 MB

english, 2013

11

Inhibition of the Human Proteasome by Imidazoline Scaffolds

Azevedo, Lauren M., Lansdell, Theresa A., Ludwig, Jacob R., Mosey, Robert A., Woloch, Daljinder K., Cogan, Dillon P., Patten, Gregory P., Kuszpit, Michael R., Fisk, Jason S., Tepe, Jetze J.

Journal:

Journal of Medicinal Chemistry

Year:

2013

Language:

english

File:

PDF, 342 KB

english, 2013

12

2-[(3a R ,4 R ,5 S ,7a S )-5-{(1 S )-1-[3,5-Bis(trifluoromethyl)phenyl]-2-hydroxyethoxy}-4-(2-methylphenyl)octahydro-2 H -isoindol-2-yl]-1,3-oxazol-4(5 H )-one: A Potent Human NK 1 Receptor Antagonist with Multiple Clearance Pathways

Kassick, Andrew J., Jiang, Jinlong, Bunda, Jaime, Wilson, David, Bao, Jianming, Lu, Huagang, Lin, Peter, Ball, Richard G., Doss, George A., Tong, Xinchun, Tsao, Kwei-Lan C., Wang, Hong, Chicchi, Gary,

Journal:

Journal of Medicinal Chemistry

Year:

2013

Language:

english

File:

PDF, 949 KB

english, 2013

13

Design, Synthesis, and Evaluation of Multitarget-Directed Resveratrol Derivatives for the Treatment of Alzheimer’s Disease

Lu, Chuanjun, Guo, Yueyan, Yan, Jun, Luo, Zonghua, Luo, Hai-Bin, Yan, Ming, Huang, Ling, Li, Xingshu

Journal:

Journal of Medicinal Chemistry

Year:

2013

Language:

english

File:

PDF, 956 KB

english, 2013

14

LDK378: A Promising Anaplastic Lymphoma Kinase (ALK) Inhibitor

Chen, Jianyong, Jiang, Cheng, Wang, Shaomeng

Journal:

Journal of Medicinal Chemistry

Year:

2013

Language:

english

File:

PDF, 215 KB

english, 2013

15

Targeting Gain of Function and Resistance Mutations in Abl and KIT by Hybrid Compound Design

Richters, André, Ketzer, Julia, Getlik, Matthäus, Grütter, Christian, Schneider, Ralf, Heuckmann, Johannes M., Heynck, Stefanie, Sos, Martin L., Gupta, Anu, Unger, Anke, Schultz-Fademrecht, Carsten, T

Journal:

Journal of Medicinal Chemistry

Year:

2013

Language:

english

File:

PDF, 4.49 MB

english, 2013

16

Development of Polyamine Transport Ligands with Improved Metabolic Stability and Selectivity against Specific Human Cancers

Muth, Aaron, Kamel, Joseph, Kaur, Navneet, Shicora, Allyson C., Ayene, Iraimoudi S., Gilmour, Susan K., Phanstiel, Otto

Journal:

Journal of Medicinal Chemistry

Year:

2013

Language:

english

File:

PDF, 563 KB

english, 2013

17

Design and Development of Stable, Water-Soluble, Human Toll-like Receptor 2 Specific Monoacyl Lipopeptides as Candidate Vaccine Adjuvants

Salunke, Deepak B., Connelly, Seth W., Shukla, Nikunj M., Hermanson, Alec R., Fox, Lauren M., David, Sunil A.

Journal:

Journal of Medicinal Chemistry

Year:

2013

Language:

english

File:

PDF, 1.77 MB

english, 2013

18

4-Amino-7-chloroquinolines: Probing Ligand Efficiency Provides Botulinum Neurotoxin Serotype A Light Chain Inhibitors with Significant Antiprotozoal Activity

Opsenica, Igor M., Tot, Mikloš, Gomba, Laura, Nuss, Jonathan E., Sciotti, Richard J., Bavari, Sina, Burnett, James C., Šolaja, Bogdan A.

Journal:

Journal of Medicinal Chemistry

Year:

2013

Language:

english

File:

PDF, 578 KB

english, 2013

19

Discovery of RG7388, a Potent and Selective p53–MDM2 Inhibitor in Clinical Development

Ding, Qingjie, Zhang, Zhuming, Liu, Jin-Jun, Jiang, Nan, Zhang, Jing, Ross, Tina M., Chu, Xin-Jie, Bartkovitz, David, Podlaski, Frank, Janson, Cheryl, Tovar, Christian, Filipovic, Zoran M., Higgins, B

Journal:

Journal of Medicinal Chemistry

Year:

2013

Language:

english

File:

PDF, 1.76 MB

english, 2013

20

Synthesis and Structure–Activity Relationship Studies of O -Biphenyl-3-yl Carbamates as Peripherally Restricted Fatty Acid Amide Hydrolase Inhibitors

Moreno-Sanz, Guillermo, Duranti, Andrea, Melzig, Laurin, Fiorelli, Claudio, Ruda, Gian Filippo, Colombano, Giampiero, Mestichelli, Paola, Sanchini, Silvano, Tontini, Andrea, Mor, Marco, Bandiera, Tizi

Journal:

Journal of Medicinal Chemistry

Year:

2013

Language:

english

File:

PDF, 850 KB

english, 2013

21

Carbamoyl Pyridone HIV-1 Integrase Inhibitors 3. A Diastereomeric Approach to Chiral Nonracemic Tricyclic Ring Systems and the Discovery of Dolutegravir (S/GSK1349572) and (S/GSK1265744)

Johns, Brian A., Kawasuji, Takashi, Weatherhead, Jason G., Taishi, Teruhiko, Temelkoff, David P., Yoshida, Hiroshi, Akiyama, Toshiyuki, Taoda, Yoshiyuki, Murai, Hitoshi, Kiyama, Ryuichi, Fuji, Masahir

Journal:

Journal of Medicinal Chemistry

Year:

2013

Language:

english

File:

PDF, 1.22 MB

english, 2013

22

A Class of Sulfonamides with Strong Inhibitory Action against the α-Carbonic Anhydrase from Trypanosoma cruzi

Güzel-Akdemir, Özlen, Akdemir, Atilla, Pan, Peiwen, Vermelho, Alane B., Parkkila, Seppo, Scozzafava, Andrea, Capasso, Clemente, Supuran, Claudiu T.

Journal:

Journal of Medicinal Chemistry

Year:

2013

Language:

english

File:

PDF, 2.20 MB

english, 2013

23

Discovery of Bufadienolides as a Novel Class of ClC-3 Chloride Channel Activators with Antitumor Activities

Liu, Junshan, Zhang, Dongmei, Li, Yuan, Chen, Weimin, Ruan, Zhixiong, Deng, Lijuan, Wang, Liwei, Tian, Haiyan, Yiu, Anita, Fan, Chunlin, Luo, Hai, Liu, Shanwen, Wang, Ying, Xiao, Gaokeng, Chen, Lixin,

Journal:

Journal of Medicinal Chemistry

Year:

2013

Language:

english

File:

PDF, 1.60 MB

english, 2013

24

Investigation of the Noncovalent Binding Mode of Covalent Proteasome Inhibitors around the Transition State by Combined Use of Cyclopropylic Strain-Based Conformational Restriction and Computational Modeling

Kawamura, Shuhei, Unno, Yuka, Tanaka, Motohiro, Sasaki, Takuma, Yamano, Akihito, Hirokawa, Takatsugu, Kameda, Tomoshi, Asai, Akira, Arisawa, Mitsuhiro, Shuto, Satoshi

Journal:

Journal of Medicinal Chemistry

Year:

2013

Language:

english

File:

PDF, 4.64 MB

english, 2013

25

Synthesis and in Vitro Photodynamic Activity of Oligomeric Ethylene Glycol–Quinoline Substituted Zinc(II) Phthalocyanine Derivatives

Jia, Xiao, Yang, Feng-Feng, Li, Jun, Liu, Jian-Yong, Xue, Jin-Ping

Journal:

Journal of Medicinal Chemistry

Year:

2013

Language:

english

File:

PDF, 2.39 MB

english, 2013

26

Cyclic Enkephalins with a Diversely Substituted Guanidine Bridge or a Thiourea Bridge: Synthesis, Biological and Structural Evaluations

Touati-Jallabe, Youness, Bojnik, Engin, Legrand, Baptiste, Mauchauffée, Elodie, Chung, Nga N., Schiller, Peter W., Benyhe, Sandor, Averlant-Petit, Marie-Christine, Martinez, Jean, Hernandez, Jean-Fran

Journal:

Journal of Medicinal Chemistry

Year:

2013

Language:

english

File:

PDF, 633 KB

english, 2013

27

Synthesis and Biological Properties of Novel Brefeldin A Analogues

Seehafer, Kai, Rominger, Frank, Helmchen, Günter, Langhans, Markus, Robinson, David G., Özata, Başak, Brügger, Britta, Strating, Jeroen R. P. M., van Kuppeveld, Frank J. M., Klein, Christian D.

Journal:

Journal of Medicinal Chemistry

Year:

2013

Language:

english

File:

PDF, 4.69 MB

english, 2013

28

Atropisomeric 4-Phenyl-4 H -1,2,4-triazoles as Selective Glycine Transporter 1 Inhibitors

Sugane, Takashi, Tobe, Takahiko, Hamaguchi, Wataru, Shimada, Itsuro, Maeno, Kyoichi, Miyata, Junji, Suzuki, Takeshi, Kimizuka, Tetsuya, Sakamoto, Shuichi, Tsukamoto, Shin-ichi

Journal:

Journal of Medicinal Chemistry

Year:

2013

Language:

english

File:

PDF, 1.34 MB

english, 2013

29

Correction to Chemoenzymatic Synthesis of New 2,4- syn -Functionalized ( S )-Glutamate Analogues and Structure–Activity Relationship Studies at Ionotropic Glutamate Receptors and Excitatory Amino Acid Transporters

Assaf, Zeinab, Larsen, Anja P., Venskutonytė, Raminta, Han, Liwei, Abrahamsen, Bjarke, Nielsen, Birgitte, Gajhede, Michael, Kastrup, Jette S., Jensen, Anders A., Pickering, Darryl S., Frydenvang, Karl

Journal:

Journal of Medicinal Chemistry

Year:

2013

Language:

english

File:

PDF, 121 KB

english, 2013

30

Correction to Structure–Activity Relationship of N,N′-Disubstituted Pyrimidinetriones as Ca V 1.3 Calcium Channel-Selective Antagonists for Parkinson’s Disease

Kang, Soosung, Cooper, Garry, Dunne, Sara Fernandez, Luan, Chi-Hao, Surmeier, D. James, Silverman, Richard B.

Journal:

Journal of Medicinal Chemistry

Year:

2013

File:

PDF, 127 KB

2013

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