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Page 1
The development and SAR of pyrrolidine carboxamide 11beta-HSD1 inhibitors.
Cheng H, Hoffman J, Le P, Nair SK, Cripps S, Matthews J, Smith C, Yang M, Kupchinsky S, Dress K, Edwards M, Cole B, Walters E, Loh C, Ermolieff J, Fanjul A, Bhat GB, Herrera J, Pauly T, Hosea N, Paderes G, Rejto P. Cheng H, et al. Bioorg Med Chem Lett. 2010 May 1;20(9):2897-902. doi: 10.1016/j.bmcl.2010.03.032. Epub 2010 Mar 10. Bioorg Med Chem Lett. 2010. PMID: 20363126
Discovery of a novel class of exquisitely selective mesenchymal-epithelial transition factor (c-MET) protein kinase inhibitors and identification of the clinical candidate 2-(4-(1-(quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl)-1H-pyrazol-1-yl)ethanol (PF-04217903) for the treatment of cancer.
Cui JJ, McTigue M, Nambu M, Tran-Dubé M, Pairish M, Shen H, Jia L, Cheng H, Hoffman J, Le P, Jalaie M, Goetz GH, Ryan K, Grodsky N, Deng YL, Parker M, Timofeevski S, Murray BW, Yamazaki S, Aguirre S, Li Q, Zou H, Christensen J. Cui JJ, et al. J Med Chem. 2012 Sep 27;55(18):8091-109. doi: 10.1021/jm300967g. Epub 2012 Sep 10. J Med Chem. 2012. PMID: 22924734
The discovery and structure-activity relationships leading to CE-156811, a difluorophenyl cyclopropyl fluoroether: a novel potent antibacterial analog derived from hygromycin A.
Le PT, Brickner SJ, Wade SK, Brighty K, Monahan R, Stone GG, Girard D, Finegan S, Duignan J, Schafer J, Maloney M, Zaniewski RP, Connolly AG, Liras J, Bordner J, Samardjiev I. Le PT, et al. Bioorg Med Chem Lett. 2011 Jan 1;21(1):276-9. doi: 10.1016/j.bmcl.2010.11.022. Epub 2010 Nov 10. Bioorg Med Chem Lett. 2011. PMID: 21115249
Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain exposure and broad-spectrum potency against ALK-resistant mutations.
Johnson TW, Richardson PF, Bailey S, Brooun A, Burke BJ, Collins MR, Cui JJ, Deal JG, Deng YL, Dinh D, Engstrom LD, He M, Hoffman J, Hoffman RL, Huang Q, Kania RS, Kath JC, Lam H, Lam JL, Le PT, Lingardo L, Liu W, McTigue M, Palmer CL, Sach NW, Smeal T, Smith GL, Stewart AE, Timofeevski S, Zhu H, Zhu J, Zou HY, Edwards MP. Johnson TW, et al. Among authors: le pt. J Med Chem. 2014 Jun 12;57(11):4720-44. doi: 10.1021/jm500261q. Epub 2014 Jun 3. J Med Chem. 2014. PMID: 24819116
Synthesis and biological evaluation of novel hygromycin A antibacterial agents.
Visser MS, Freeman-Cook KD, Brickner SJ, Brighty KE, Le PT, Wade SK, Monahan R, Martinelli GJ, Blair KT, Moore DE. Visser MS, et al. Among authors: le pt. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6730-4. doi: 10.1016/j.bmcl.2010.08.139. Epub 2010 Sep 21. Bioorg Med Chem Lett. 2010. PMID: 20864341
Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib.
Huang Q, Johnson TW, Bailey S, Brooun A, Bunker KD, Burke BJ, Collins MR, Cook AS, Cui JJ, Dack KN, Deal JG, Deng YL, Dinh D, Engstrom LD, He M, Hoffman J, Hoffman RL, Johnson PS, Kania RS, Lam H, Lam JL, Le PT, Li Q, Lingardo L, Liu W, Lu MW, McTigue M, Palmer CL, Richardson PF, Sach NW, Shen H, Smeal T, Smith GL, Stewart AE, Timofeevski S, Tsaparikos K, Wang H, Zhu H, Zhu J, Zou HY, Edwards MP. Huang Q, et al. Among authors: le pt. J Med Chem. 2014 Feb 27;57(4):1170-87. doi: 10.1021/jm401805h. Epub 2014 Feb 6. J Med Chem. 2014. PMID: 24432909 Free article.
In vitro antibacterial activity of CE-156811, a novel analog derived from hygromycin A.
Stone GG, Girard D, Finegan S, Duignan J, Schafer J, Maloney M, Zaniewski RP, Brickner SJ, Wade SK, Le PT, Huband MD. Stone GG, et al. Among authors: le pt. Antimicrob Agents Chemother. 2008 Jul;52(7):2663-6. doi: 10.1128/AAC.01326-07. Epub 2008 Apr 21. Antimicrob Agents Chemother. 2008. PMID: 18426902 Free PMC article.
193 results