Volume 5; Issue 4

ACS Medicinal Chemistry Letters

Volume 5; Issue 4

1

Plasmepsin Inhibitory Activity and Structure-Guided Optimization of a Potent Hydroxyethylamine-Based Antimalarial Hit

Jaudzems, Kristaps, Tars, Kaspars, Maurops, Gundars, Ivdra, Natalija, Otikovs, Martins, Leitans, Janis, Kanepe-Lapsa, Iveta, Domraceva, Ilona, Mutule, Ilze, Trapencieris, Peteris, Blackman, Michael J.

Journal:

ACS Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 961 KB

english, 2014

2

Iron Chelators in Photodynamic Therapy Revisited: Synergistic Effect by Novel Highly Active Thiosemicarbazones

Mrozek-Wilczkiewicz, Anna, Serda, Maciej, Musiol, Robert, Malecki, Grzegorz, Szurko, Agnieszka, Muchowicz, Angelika, Golab, Jakub, Ratuszna, Alicja, Polanski, Jaroslaw

Journal:

ACS Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 343 KB

english, 2014

3

Design and Evaluation of ω-Hydroxy Fatty Acids Containing α-GalCer Analogues for CD1d-Mediated NKT Cell Activation

Lim, Chaemin, Kim, Jae Hyun, Baek, Dong Jae, Lee, Joo-Youn, Cho, Minjae, Lee, Yoon-Sook, Kang, Chang-Yuil, Chung, Doo Hyun, Cho, Won-Jae, Kim, Sanghee

Journal:

ACS Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 1.21 MB

english, 2014

4

3-Amido-3-aryl-piperidines: A Novel Class of Potent, Selective, and Orally Active GlyT1 Inhibitors

Pinard, Emmanuel, Alberati, Daniela, Alvarez-Sanchez, Ruben, Brom, Virginie, Burner, Serge, Fischer, Holger, Hauser, Nicole, Kolczewski, Sabine, Lengyel, Judith, Mory, Roland, Saladin, Christian, Schu

Journal:

ACS Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 915 KB

english, 2014

5

R -Configuration of 4-Aminopyridyl-Based Inhibitors of CYP51 Confers Superior Efficacy Against Trypanosoma cruzi

Choi, Jun Yong, Calvet, Claudia M., Vieira, Debora F., Gunatilleke, Shamila S., Cameron, Michael D., McKerrow, James H., Podust, Larissa M., Roush, William R.

Journal:

ACS Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 1.95 MB

english, 2014

6

Triazolo[4,5-d]pyrimidine Derivatives as Inhibitors of GCN2

Brazeau, Jean-Francois, Rosse, Gerard

Journal:

ACS Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 158 KB

english, 2014

7

Optimizing the Physicochemical Properties of Raf/MEK Inhibitors by Nitrogen Scanning

Aoki, Toshihiro, Hyohdoh, Ikumi, Furuichi, Noriyuki, Ozawa, Sawako, Watanabe, Fumio, Matsushita, Masayuki, Sakaitani, Masahiro, Morikami, Kenji, Takanashi, Kenji, Harada, Naoki, Tomii, Yasushi, Shirak

Journal:

ACS Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 578 KB

english, 2014

8

C-Ring Cannabinoid Lactones: A Novel Cannabinergic Chemotype

Sharma, Rishi, Nikas, Spyros P., Guo, Jason Jianxin, Mallipeddi, Srikrishnan, Wood, JodiAnne T., Makriyannis, Alexandros

Journal:

ACS Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 999 KB

english, 2014

9

In Vitro Membrane Permeation Studies and in Vivo Antinociception of Glycosylated Dmt 1 -DALDA Analogues

Ballet, Steven, Betti, Cecilia, Novoa, Alexandre, Tömböly, Csaba, Uhd Nielsen, Carsten, Helms, Hans Christian, Lesniak, Anna, Kleczkowska, Patrycja, Chung, Nga N., Lipkowski, Andrzej W., Brodin, Birge

Journal:

ACS Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 675 KB

english, 2014

10

A New Challenging and Promising Era of Tyrosine Kinase Inhibitors

Journal:

ACS Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 702 KB

english, 2014

11

Phenyl Carboxamide Analogues as Spleen Tyrosine Kinase (Syk) Inhibitors

Brazeau, Jean-Francois, Rosse, Gerard

Journal:

ACS Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 217 KB

english, 2014

12

Novel Cycloalkenepyrazoles as Inhibitors of Bub1 Kinase

Brazeau, Jean-Francois, Rosse, Gerard

Journal:

ACS Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 268 KB

english, 2014

13

Multicolor Imaging of Endoplasmic Reticulum-Located Esterase As a Prodrug Activation Enzyme

Hakamata, Wataru, Tamura, Saori, Hirano, Takako, Nishio, Toshiyuki

Journal:

ACS Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 1007 KB

english, 2014

14

Delayed and Prolonged Histone Hyperacetylation with a Selective HDAC1/HDAC2 Inhibitor

Methot, Joey L., Hoffman, Dawn Mampreian, Witter, David J., Stanton, Matthew G., Harrington, Paul, Hamblett, Christopher, Siliphaivanh, Phieng, Wilson, Kevin, Hubbs, Jed, Heidebrecht, Richard, Kral, A

Journal:

ACS Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 964 KB

english, 2014

15

Novel 2,4-Diarylaminopyrimidine Analogues (DAAPalogues) Showing Potent c-Met/ALK Multikinase Inhibitory Activities

Liu, Zhiqing, Ai, Jing, Peng, Xia, Song, Zilan, Wu, Kui, Zhang, Jing, Yao, Qizheng, Chen, Yi, Ji, Yinchun, Yang, Yanhong, Geng, Meiyu, Zhang, Ao

Journal:

ACS Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 731 KB

english, 2014

16

Improving the Pharmacokinetics of GPR40/FFA1 Full Agonists

Du, Xiaohui, Dransfield, Paul J., Lin, Daniel C.-H., Wong, Simon, Wang, Yingcai, Wang, Zhongyu, Kohn, Todd, Yu, Ming, Brown, Sean P., Vimolratana, Marc, Zhu, Liusheng, Li, An-Rong, Su, Yongli, Jiao, X

Journal:

ACS Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 688 KB

english, 2014

17

Discovery of BI 224436, a Noncatalytic Site Integrase Inhibitor (NCINI) of HIV-1

Fader, Lee D., Malenfant, Eric, Parisien, Mathieu, Carson, Rebekah, Bilodeau, François, Landry, Serge, Pesant, Marc, Brochu, Christian, Morin, Sébastien, Chabot, Catherine, Halmos, Ted, Bousquet, Yves

Journal:

ACS Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 1.04 MB

english, 2014

18

Trifluoromethyl Fluorocoxib A Detects Cyclooxygenase-2 Expression in Inflammatory Tissues and Human Tumor Xenografts

Uddin, Md. Jashim, Crews, Brenda C., Huda, Imran, Ghebreselasie, Kebreab, Daniel, Cristina K., Marnett, Lawrence J.

Journal:

ACS Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 3.67 MB

english, 2014

19

Creation of Novel Cores for β-Secretase (BACE-1) Inhibitors: A Multiparameter Lead Generation Strategy

Viklund, Jenny, Kolmodin, Karin, Nordvall, Gunnar, Swahn, Britt-Marie, Svensson, Mats, Gravenfors, Ylva, Rahm, Fredrik

Journal:

ACS Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 1.17 MB

english, 2014

20

Discovery of AZD3199, An Inhaled Ultralong Acting β 2 Receptor Agonist with Rapid Onset of Action

Stocks, Michael J., Alcaraz, Lilian, Bailey, Andrew, Bonnert, Roger, Cadogan, Elaine, Christie, Jadeen, Dixon, John, Connolly, Stephen, Cook, Anthony, Fisher, Adrian, Flaherty, Alice, Humphries, Alexa

Journal:

ACS Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 819 KB

english, 2014

21

Minibody-Indocyanine Green Based Activatable Optical Imaging Probes: The Role of Short Polyethylene Glycol Linkers

Watanabe, Rira, Sato, Kazuhide, Hanaoka, Hirofumi, Harada, Toshiko, Nakajima, Takahito, Kim, Insook, Paik, Chang H., Wu, Anna M., Choyke, Peter L., Kobayashi, Hisataka

Journal:

ACS Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 2.38 MB

english, 2014

22

Oxathiazolones Selectively Inhibit the Human Immunoproteasome over the Constitutive Proteasome

Fan, Hao, Angelo, Nicholas G., Warren, J. David, Nathan, Carl F., Lin, Gang

Journal:

ACS Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 1.33 MB

english, 2014

23

Digitoxin Analogues with Improved Anticytomegalovirus Activity

Cai, Hongyi, Wang, Hua-Yu L., Venkatadri, Rajkumar, Fu, De-Xue, Forman, Michael, Bajaj, Sumit O., Li, Hongyan, O’Doherty, George A., Arav-Boger, Ravit

Journal:

ACS Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 1.72 MB

english, 2014

24

Vivid Tumor Imaging Utilizing Liposome-Carried Bimodal Radiotracer

Kim, Jonghee, Pandya, Darpan N., Lee, Woonghee, Park, Jang Woo, Kim, Youn Ji, Kwak, Wonjung, Ha, Yeong Su, Chang, Yongmin, An, Gwang Il, Yoo, Jeongsoo

Journal:

ACS Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 2.36 MB

english, 2014

25

Discovery and Optimization of Tetramethylpiperidinyl Benzamides as Inhibitors of EZH2

Nasveschuk, Christopher G., Gagnon, Alexandre, Garapaty-Rao, Shivani, Balasubramanian, Srividya, Campbell, Robert, Lee, Christina, Zhao, Feng, Bergeron, Louise, Cummings, Richard, Trojer, Patrick, Aud

Journal:

ACS Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 930 KB

english, 2014

26

Novel Delta Opioid Receptor Agonists with Oxazatricyclodecane Structure

Fujii, Hideaki, Hayashida, Kohei, Saitoh, Akiyoshi, Yokoyama, Akinobu, Hirayama, Shigeto, Iwai, Takashi, Nakata, Eriko, Nemoto, Toru, Sudo, Yuka, Uezono, Yasuhito, Yamada, Mitsuhiko, Nagase, Hiroshi

Journal:

ACS Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 726 KB

english, 2014

27

Structure–Activity Relationship of Semicarbazone EGA Furnishes Photoaffinity Inhibitors of Anthrax Toxin Cellular Entry

Jung, Michael E., Chamberlain, Brian T., Ho, Chi-Lee C., Gillespie, Eugene J., Bradley, Kenneth A.

Journal:

ACS Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 810 KB

english, 2014

28

Enhancing a CH−π Interaction to Increase the Affinity for 5-HT 1A Receptors

Liégeois, Jean-François, Lespagnard, Marc, Meneses Salas, Elsa, Mangin, Floriane, Scuvée-Moreau, Jacqueline, Dilly, Sébastien

Journal:

ACS Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 1.48 MB

english, 2014

29

Interkingdom Pharmacology of Angiotensin-I Converting Enzyme Inhibitor Phosphonates Produced by Actinomycetes

Kramer, Glenna J., Mohd, Akif, Schwager, Sylva L. U., Masuyer, Geoffrey, Acharya, K. Ravi, Sturrock, Edward D., Bachmann, Brian O.

Journal:

ACS Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 1.94 MB

english, 2014

30

Development of [ 3 H]2-Carboxy-4,6-dichloro-1 H -indole-3-propionic Acid ([ 3 H]PSB-12150): A Useful Tool for Studying GPR17

Köse, Meryem, Ritter, Kirsten, Thiemke, Katharina, Gillard, Michel, Kostenis, Evi, Müller, Christa E.

Journal:

ACS Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 607 KB

english, 2014

31

Discovery of Short Peptides Exhibiting High Potency against Cryptococcus neoformans

Mahindra, Amit, Bagra, Nitin, Wangoo, Nishima, Khan, Shabana I., Jacob, Melissa R., Jain, Rahul

Journal:

ACS Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 2.59 MB

english, 2014

32

Discovery and Biological Evaluation of Novel Dual EGFR/c-Met Inhibitors

Szokol, Bálint, Gyulavári, Pál, Kurkó, Ibolya, Baska, Ferenc, Szántai-Kis, Csaba, Greff, Zoltán, Őrfi, Zoltán, Peták, István, Pénzes, Kinga, Torka, Robert, Ullrich, Axel, Őrfi, László, Vántus, Tibor,

Journal:

ACS Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 2.36 MB

english, 2014

33

Analogues of the Natural Product Sinefungin as Inhibitors of EHMT1 and EHMT2

Devkota, Kanchan, Lohse, Brian, Liu, Qing, Wang, Ming-Wei, Stærk, Dan, Berthelsen, Jens, Clausen, Rasmus Prætorius

Journal:

ACS Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 518 KB

english, 2014

34

Liver S9 Fraction-Derived Metabolites of Curcumin Analogue UBS109

Moore, Terry W., Zhu, Shijun, Randolph, Ryan, Shoji, Mamoru, Snyder, James P.

Journal:

ACS Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 643 KB

english, 2014

35

Thiazolocarboxamide Analogues as NAMPT Inhibitors

Brazeau, Jean-Francois, Rosse, Gerard

Journal:

ACS Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 191 KB

english, 2014

36

Corrrection to Discovery of Tetrahydropyrazolopyrimidine Carboxamide Derivatives As Potent and Orally Active Novel Antitubercular Agents

Yokokawa, Fumiaki, Wang, Gang, Chan, Wai Ling, Ang, Shi Hua, Wong, Josephine, Ma, Ida, Rao, Srinivasa P S, Manjunatha, Ujjini, Lakshminarayana, Suresh B, Herve, Maxime, Kounde, Cyrille, Tan, Bee Huat,

Journal:

ACS Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 121 KB

english, 2014

37

In This Issue, Volume 5, Issue 4

Silverman, Janice Elaine Y.

Journal:

ACS Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 653 KB

english, 2014

38

Selective 5-HT Receptor Modulators May Deliver Focused Targeting with Fewer Adverse Effects

Abdel-Magid, Ahmed F.

Journal:

ACS Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 238 KB

english, 2014

39

Inhibitors of Factor XIa and Plasma Kallikrein May Treat Thromboembolic Disorders and Many Diabetes Complications

Abdel-Magid, Ahmed F.

Journal:

ACS Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 264 KB

english, 2014

40

Quinoline Derivatives as 5-HT 6 Receptor PET Ligands

Journal:

ACS Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 204 KB

english, 2014

41

New Frontiers in Kinases: Special Issue

Botta, Maurizio

Journal:

ACS Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 130 KB

english, 2014

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