Volume 6; Issue 5

ACS Medicinal Chemistry Letters

Volume 6; Issue 5

1

Design, Synthesis, and Biological Evaluation of Novel Imidazo[1,2- a ]pyridine Derivatives as Potent c-Met Inhibitors

Li, Chunpu, Ai, Jing, Zhang, Dengyou, Peng, Xia, Chen, Xi, Gao, Zhiwei, Su, Yi, Zhu, Wei, Ji, Yinchun, Chen, Xiaoyan, Geng, Meiyu, Liu, Hong

Journal:

ACS Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 309 KB

english, 2015

2

( R )-2-Phenylpyrrolidine Substituted Imidazopyridazines: A New Class of Potent and Selective Pan-TRK Inhibitors

Choi, Ha-Soon, Rucker, Paul V., Wang, Zhicheng, Fan, Yi, Albaugh, Pamela, Chopiuk, Greg, Gessier, Francois, Sun, Fangxian, Adrian, Francisco, Liu, Guoxun, Hood, Tami, Li, Nanxin, Jia, Yong, Che, Jianw

Journal:

ACS Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 1.42 MB

english, 2015

3

N -(3-Ethynyl-2,4-difluorophenyl)sulfonamide Derivatives as Selective Raf Inhibitors

Li, Yingjun, Cheng, Huimin, Zhang, Zhang, Zhuang, Xiaoxi, Luo, Jinfeng, Long, Huoyou, Zhou, Yang, Xu, Yong, Taghipouran, Rana, Li, Dan, Patterson, Adam, Smaill, Jeff, Tu, Zhengchao, Wu, Donghai, Ren,

Journal:

ACS Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 1.75 MB

english, 2015

4

Synthesis and Initial in Vivo Studies with [ 11 C]SB-216763: The First Radiolabeled Brain Penetrative Inhibitor of GSK-3

Li, Lei, Shao, Xia, Cole, Erin L., Ohnmacht, Stephan A., Ferrari, Valentina, Hong, Young T., Williamson, David J., Fryer, Tim D., Quesada, Carole A., Sherman, Phillip, Riss, Patrick J., Scott, Peter J

Journal:

ACS Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 1.15 MB

english, 2015

5

Discovery of a Potent Class of PI3Kα Inhibitors with Unique Binding Mode via Encoded Library Technology (ELT)

Yang, Hongfang, Medeiros, Patricia F., Raha, Kaushik, Elkins, Patricia, Lind, Kenneth E., Lehr, Ruth, Adams, Nicholas D., Burgess, Joelle L., Schmidt, Stanley J., Knight, Steven D., Auger, Kurt R., Sc

Journal:

ACS Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 719 KB

english, 2015

6

EPZ011989, A Potent, Orally-Available EZH2 Inhibitor with Robust in Vivo Activity

Campbell, John E., Kuntz, Kevin W., Knutson, Sarah K., Warholic, Natalie M., Keilhack, Heike, Wigle, Tim J., Raimondi, Alejandra, Klaus, Christine R., Rioux, Nathalie, Yokoi, Akira, Kawano, Satoshi, M

Journal:

ACS Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 1.45 MB

english, 2015

7

SAR and Structural Analysis of Siderophore-Conjugated Monocarbam Inhibitors of Pseudomonas aeruginosa PBP3

Murphy-Benenato, Kerry E., Dangel, Brian, Davis, Hajnalka E., Durand-Réville, Thomas F., Ferguson, Andrew D., Gao, Ning, Jahić, Haris, Mueller, John P., Manyak, Erika L., Quiroga, Olga, Rooney, Michae

Journal:

ACS Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 1.27 MB

english, 2015

8

Discovery of Quinazoline-Based Fluorescent Probes to α 1 -Adrenergic Receptors

Zhang, Wei, Ma, Zhao, Li, Wenhua, Li, Geng, Chen, Laizhong, Liu, Zhenzhen, Du, Lupei, Li, Minyong

Journal:

ACS Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 1.49 MB

english, 2015

9

Design and Evaluation of 3-(Benzylthio)benzamide Derivatives as Potent and Selective SIRT2 Inhibitors

Khanfar, Mohammad A., Quinti, Luisa, Wang, Hua, Nobles, Johnathan, Kazantsev, Aleksey G., Silverman, Richard B.

Journal:

ACS Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 1.90 MB

english, 2015

10

Design and Validation of FRESH, a Drug Discovery Paradigm Resting on Robust Chemical Synthesis

Shi, Qi, Kaiser, Thomas M., Dentmon, Zackery W., Ceruso, Mariangela, Vullo, Daniela, Supuran, Claudiu T., Snyder, James P.

Journal:

ACS Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 411 KB

english, 2015

11

Design, Synthesis, and Pharmacological Evaluation of Fused β-Homophenylalanine Derivatives as Potent DPP-4 Inhibitors

Jiang, Tao, Zhou, Yuren, Chen, Zhuxi, Sun, Peng, Zhu, Jianming, Zhang, Qiang, Wang, Zhen, Shao, Qiang, Jiang, Xiangrui, Li, Bo, Chen, Kaixian, Jiang, Hualiang, Wang, Heyao, Zhu, Weiliang, Shen, Jingsh

Journal:

ACS Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 1.83 MB

english, 2015

12

Inhibitors of the PD-1/PD-L1 Pathway Can Mobilize the Immune System: An Innovative Potential Therapy for Cancer and Chronic Infections

Abdel-Magid, Ahmed F.

Journal:

ACS Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 238 KB

english, 2015

13

Bis -Arylidene Oxindole–Betulinic Acid Conjugate: A Fluorescent Cancer Cell Detector with Potent Anticancer Activity

Pal, Abhishek, Ganguly, Anirban, Chowdhuri, Sumit, Yousuf, Md, Ghosh, Avijit, Barui, Ayan Kumar, Kotcherlakota, Rajesh, Adhikari, Susanta, Banerjee, Rajkumar

Journal:

ACS Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 1.35 MB

english, 2015

14

Synthesis and Pharmacology of α/β 3 -Peptides Based on the Melanocortin Agonist Ac-His- d Phe-Arg-Trp-NH 2 Sequence

Singh, Anamika, Tala, Srinivasa R., Flores, Viktor, Freeman, Katie, Haskell-Luevano, Carrie

Journal:

ACS Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 716 KB

english, 2015

15

Simple Methods for Tracking Stem Cells with 64 Cu-Labeled DOTA-hexadecyl-benzoate

Kim, Min Hwan, Woo, Sang-Keun, Kim, Kwang Il, Lee, Tae Sup, Kim, Chan Wha, Kang, Joo Hyun, Kim, Byung Il, Lim, Sang Moo, Lee, Kyo Chul, Lee, Yong Jin

Journal:

ACS Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 1.36 MB

english, 2015

16

Discovery of Clinical Candidate BMS-906024: A Potent Pan-Notch Inhibitor for the Treatment of Leukemia and Solid Tumors

Gavai, Ashvinikumar V., Quesnelle, Claude, Norris, Derek, Han, Wen-Ching, Gill, Patrice, Shan, Weifang, Balog, Aaron, Chen, Ke, Tebben, Andrew, Rampulla, Richard, Wu, Dauh-Rurng, Zhang, Yingru, Mathur

Journal:

ACS Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 448 KB

english, 2015

17

Discovery of a Pyrrolopyrimidine (JH-II-127), a Highly Potent, Selective, and Brain Penetrant LRRK2 Inhibitor

Hatcher, John M., Zhang, Jinwei, Choi, Hwan Geun, Ito, Genta, Alessi, Dario R., Gray, Nathanael S.

Journal:

ACS Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 2.95 MB

english, 2015

18

Discovery of a Potent Parenterally Administered Factor XIa Inhibitor with Hydroxyquinolin-2(1 H )-one as the P2′ Moiety

Hu, Zilun, Wong, Pancras C., Gilligan, Paul J., Han, Wei, Pabbisetty, Kumar B., Bozarth, Jeffrey M., Crain, Earl J., Harper, Timothy, Luettgen, Joseph M., Myers, Joseph E., Ramamurthy, Vidhyashankar,

Journal:

ACS Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 1.62 MB

english, 2015

19

Design of Pyridopyrazine-1,6-dione γ-Secretase Modulators that Align Potency, MDR Efflux Ratio, and Metabolic Stability

Pettersson, Martin, Johnson, Douglas S., Humphrey, John M., Butler, Todd W., am Ende, Christopher W., Fish, Benjamin A., Green, Michael E., Kauffman, Gregory W., Mullins, Patrick B., O’Donnell, Christ

Journal:

ACS Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 466 KB

english, 2015

20

Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes

Shah, Shrenik K., He, Shuwen, Guo, Liangqin, Truong, Quang, Qi, Hongbo, Du, Wu, Lai, Zhong, Liu, Jian, Jian, Tianying, Hong, Qingmei, Dobbelaar, Peter, Ye, Zhixiong, Sherer, Edward, Feng, Zhe, Yu, Yan

Journal:

ACS Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 1.84 MB

english, 2015

21

Synthesis of Mixed Opioid Affinity Cyclic Endomorphin-2 Analogues with Fluorinated Phenylalanines

Piekielna, Justyna, Perlikowska, Renata, do-Rego, Jean Claude, do-Rego, Jean-Luc, Cerlesi, Maria Camilla, Calo, Girolamo, Kluczyk, Alicja, Łapiński, Krzysztof, Tömböly, Csaba, Janecka, Anna

Journal:

ACS Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 470 KB

english, 2015

22

Discovery of Benzimidazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys

Hoyt, Scott B., Park, Min K., London, Clare, Xiong, Yusheng, Tata, Jim, Bennett, D. Jonathan, Cooke, Andrew, Cai, Jiaqiang, Carswell, Emma, Robinson, John, MacLean, John, Brown, Lindsay, Belshaw, Simo

Journal:

ACS Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 356 KB

english, 2015

23

Inhibitors of the PAR-2 Signaling Pathway May Treat Pain and Inflammation

Abdel-Magid, Ahmed F.

Journal:

ACS Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 250 KB

english, 2015

24

Antagonism/Agonism Modulation to Build Novel Antihypertensives Selectively Triggering I 1 -Imidazoline Receptor Activation

Del Bello, Fabio, Bargelli, Valentina, Cifani, Carlo, Gratteri, Paola, Bazzicalupi, Carla, Diamanti, Eleonora, Giannella, Mario, Mammoli, Valerio, Matucci, Rosanna, Micioni Di Bonaventura, Maria Vitto

Journal:

ACS Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 1.27 MB

english, 2015

25

Monocarboxylate Transporter 1 Inhibitors as Potential Anticancer Agents

Gurrapu, Shirisha, Jonnalagadda, Sravan K., Alam, Mohammad A., Nelson, Grady L., Sneve, Mary G., Drewes, Lester R., Mereddy, Venkatram R.

Journal:

ACS Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 584 KB

english, 2015

26

Improved Stability of Proline-Derived Direct Thrombin Inhibitors through Hydroxyl to Heterocycle Replacement

Chobanian, Harry R., Pio, Barbara, Guo, Yan, Shen, Hong, Huffman, Mark A., Madeira, Maria, Salituro, Gino, Terebetski, Jenna L., Ormes, James, Jochnowitz, Nina, Hoos, Lizbeth, Zhou, Yuchen, Lewis, Dal

Journal:

ACS Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 498 KB

english, 2015

27

In This Issue, Volume 6, Issue 5

Silverman, Janice Elaine Y.

Journal:

ACS Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 707 KB

english, 2015