Volume 3; Issue 5

ACS Medicinal Chemistry Letters

Volume 3; Issue 5

1

Novel Carboxamide-Based Allosteric MEK Inhibitors: Discovery and Optimization Efforts toward XL518 (GDC-0973)

Rice, Kenneth D., Aay, Naing, Anand, Neel K., Blazey, Charles M., Bowles, Owen J., Bussenius, Joerg, Costanzo, Simona, Curtis, Jeffry K., Defina, Steven C., Dubenko, Larisa

Journal:

ACS Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 1.74 MB

english, 2012

2

The Rhodadyns, a New Class of Small Molecule Inhibitors of Dynamin GTPase Activity

Robertson, Mark J., Hadzic, Gordana, Ambrus, Joseph, Pomè, D. Yuri, Hyde, Emily, Whiting, Ainslie, Mariana, Anna, von Kleist, Lisa, Chau, Ngoc, Haucke, Volker

Journal:

ACS Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 1.47 MB

english, 2012

3

Design of a Potent CB1 Receptor Antagonist Series: Potential Scaffold for Peripherally-Targeted Agents

Dow, Robert L., Carpino, Philip A., Gautreau, Denise, Hadcock, John R., Iredale, Philip A., Kelly-Sullivan, Dawn, Lizano, Jeffrey S., O’Connor, Rebecca E., Schneider, Steven R., Scott, Dennis O.

Journal:

ACS Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 911 KB

english, 2012

4

Small Molecule Suppression of Carbapenem Resistance in NDM-1 Producing Klebsiella pneumoniae

Worthington, Roberta J., Bunders, Cynthia A., Reed, Catherine S., Melander, Christian

Journal:

ACS Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 219 KB

english, 2012

5

HIV-1 Integrase Inhibitor-Inspired Antibacterials Targeting Isoprenoid Biosynthesis

Zhang, Yonghui, Lin, Fu-Yang, Li, Kai, Zhu, Wei, Liu, Yi-Liang, Cao, Rong, Pang, Ran, Lee, Eunhae, Axelson, Jordan, Hensler, Mary

Journal:

ACS Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 2.07 MB

english, 2012

6

Evolution of a Compact Photoprobe for the Dopamine Transporter Based on (±)-threo-Methylphenidate

Lapinsky, David J., Yarravarapu, Nageswari, Nolan, Tammy L., Surratt, Christopher K., Lever, John R., Tomlinson, Michael, Vaughan, Roxanne A., Deutsch, Howard M.

Journal:

ACS Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 388 KB

english, 2012

7

Anti-inflammatory Effect of a Cell-Penetrating Peptide Targeting the Nrf2/Keap1 Interaction

Steel, Richard, Cowan, Jonathan, Payerne, Estelle, O'Connell, Maria A., Searcey, Mark

Journal:

ACS Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 2.86 MB

english, 2012

8

A Divergent SAR Study Allows Optimization of a Potent 5-HT 2c Inhibitor to a Promising Antimalarial Scaffold

Calderón, Félix, Vidal-Mas, Jaume, Burrows, Jeremy, de la Rosa, Juan Carlos, Jiménez-Díaz, María Belén, Mulet, Teresa, Prats, Sara, Solana, Jorge, Witty, Michael, Gamo, Francisco Javier, Fernández, Es

Journal:

ACS Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 320 KB

english, 2012

9

Discovery of Selective Small Molecule ROMK Inhibitors as Potential New Mechanism Diuretics

Tang, Haifeng, Walsh, Shawn P., Yan, Yan, de Jesus, Reynalda K., Shahripour, Aurash, Teumelsan, Nardos, Zhu, Yuping, Ha, Sookhee, Owens, Karen A., Thomas-Fowlkes, Brande S., Felix, John P., Liu, Jessi

Journal:

ACS Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 624 KB

english, 2012

10

RXR Partial Agonist CBt-PMN Exerts Therapeutic Effects on Type 2 Diabetes without the Side Effects of RXR Full Agonists

Kakuta, Hiroki, Yakushiji, Nobumasa, Shinozaki, Ryosuke, Ohsawa, Fuminori, Yamada, Shoya, Ohta, Yui, Kawata, Kohei, Nakayama, Mariko, Hagaya, Manabu, Fujiwara, Chisa, Makishima, Makoto, Uno, Shigeyuki

Journal:

ACS Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 1.73 MB

english, 2012

11

Water-Soluble Progesterone Analogues Are Effective, Injectable Treatments in Animal Models of Traumatic Brain Injury

Guthrie, David B., Stein, Donald G., Liotta, Dennis C., Lockwood, Mark A., Sayeed, Iqbal, Atif, Fahim, Arrendale, Richard F., Reddy, G. Prabhakar, Evers, Taylor J., Marengo, Jose R., Howard, Randy B.,

Journal:

ACS Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 848 KB

english, 2012

12

In This Issue, Vol. 3, Issue 5

Silverman, Janice Elaine Y.

Journal:

ACS Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 1.90 MB

english, 2012

13

Intestinally Targeted Diacylglycerol Acyltransferase 1 (DGAT1) Inhibitors Robustly Suppress Postprandial Triglycerides

Serrano-Wu, Michael H., Coppola, Gary M., Gong, Yongjin, Neubert, Alan D., Chatelain, Ricardo, Clairmont, Kevin B., Commerford, Renee, Cosker, Theresa, Daniels, Thomas, Hou, Ying, Jain, Monish, Juedes

Journal:

ACS Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 515 KB

english, 2012

14

Targeted Kinase Selectivity from Kinase Profiling Data

Milletti, Francesca, Hermann, Johannes C.

Journal:

ACS Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 2.01 MB

english, 2012

15

β-Lactones Inhibit N -acylethanolamine Acid Amidase by S-Acylation of the Catalytic N-Terminal Cysteine

Armirotti, Andrea, Romeo, Elisa, Ponzano, Stefano, Mengatto, Luisa, Dionisi, Mauro, Karacsonyi, Claudia, Bertozzi, Fabio, Garau, Gianpiero, Tarozzo, Glauco, Reggiani, Angelo, Bandiera, Tiziano, Tarzia

Journal:

ACS Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 508 KB

english, 2012

16

Inventorship and Ownership Considerations and Pitfalls with Collaborative Research

Armstrong, MaryAnne, Murphy, Gerald M.

Journal:

ACS Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 149 KB

english, 2012

17

Fungal bis-Naphthopyrones as Inhibitors of Botulinum Neurotoxin Serotype A

Cardellina, John H., Roxas-Duncan, Virginia I., Montgomery, Vicki, Eccard, Vanessa, Campbell, Yvette, Hu, Xin, Khavrutskii, Ilja, Tawa, Gregory J., Wallqvist, Anders, Gloer, James B., Phatak, Nisarga

Journal:

ACS Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 3.04 MB

english, 2012

18

Measurement of Atropisomer Racemization Kinetics Using Segmented Flow Technology

Davoren, Jennifer E., Bundesmann, Mark W., Yan, Qi T., Collantes, Elizabeth M., Mente, Scot, Nason, Deane M., Gray, David L.

Journal:

ACS Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 482 KB

english, 2012

19

Boron-Based 4-Hydroxytamoxifen Bioisosteres for Treatment of de Novo Tamoxifen Resistant Breast Cancer

Jiang, Quan, Zhong, Qiu, Zhang, Qiang, Zheng, Shilong, Wang, Guangdi

Journal:

ACS Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 1006 KB

english, 2012

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