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Page 1
Rational Design, Synthesis, and SAR of a Novel Thiazolopyrimidinone Series of Selective PI3K-beta Inhibitors.
Lin H, Schulz MJ, Xie R, Zeng J, Luengo JI, Squire MD, Tedesco R, Qu J, Erhard K, Mack JF, Raha K, Plant R, Rominger CM, Ariazi JL, Sherk CS, Schaber MD, McSurdy-Freed J, Spengler MD, Davis CB, Hardwicke MA, Rivero RA. Lin H, et al. Among authors: raha k. ACS Med Chem Lett. 2012 May 29;3(7):524-9. doi: 10.1021/ml300045b. eCollection 2012 Jul 12. ACS Med Chem Lett. 2012. PMID: 24900504 Free PMC article.
Synthesis and structure-activity relationships of imidazo[1,2-a]pyrimidin-5(1H)-ones as a novel series of beta isoform selective phosphatidylinositol 3-kinase inhibitors.
Lin H, Erhard K, Hardwicke MA, Luengo JI, Mack JF, McSurdy-Freed J, Plant R, Raha K, Rominger CM, Sanchez RM, Schaber MD, Schulz MJ, Spengler MD, Tedesco R, Xie R, Zeng JJ, Rivero RA. Lin H, et al. Among authors: raha k. Bioorg Med Chem Lett. 2012 Mar 15;22(6):2230-4. doi: 10.1016/j.bmcl.2012.01.092. Epub 2012 Feb 4. Bioorg Med Chem Lett. 2012. PMID: 22361133
Synthesis and structure-activity relationships of 1,2,4-triazolo[1,5-a]pyrimidin-7(3H)-ones as novel series of potent β isoform selective phosphatidylinositol 3-kinase inhibitors.
Sanchez RM, Erhard K, Hardwicke MA, Lin H, McSurdy-Freed J, Plant R, Raha K, Rominger CM, Schaber MD, Spengler MD, Moore ML, Yu H, Luengo JI, Tedesco R, Rivero RA. Sanchez RM, et al. Among authors: raha k. Bioorg Med Chem Lett. 2012 May 1;22(9):3198-202. doi: 10.1016/j.bmcl.2012.03.039. Epub 2012 Mar 16. Bioorg Med Chem Lett. 2012. PMID: 22475557
Discovery of a Novel 2,6-Disubstituted Glucosamine Series of Potent and Selective Hexokinase 2 Inhibitors.
Lin H, Zeng J, Xie R, Schulz MJ, Tedesco R, Qu J, Erhard KF, Mack JF, Raha K, Rendina AR, Szewczuk LM, Kratz PM, Jurewicz AJ, Cecconie T, Martens S, McDevitt PJ, Martin JD, Chen SB, Jiang Y, Nickels L, Schwartz BJ, Smallwood A, Zhao B, Campobasso N, Qian Y, Briand J, Rominger CM, Oleykowski C, Hardwicke MA, Luengo JI. Lin H, et al. Among authors: raha k. ACS Med Chem Lett. 2015 Dec 28;7(3):217-22. doi: 10.1021/acsmedchemlett.5b00214. eCollection 2016 Mar 10. ACS Med Chem Lett. 2015. PMID: 26985301 Free PMC article.
Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin.
Knight SD, Adams ND, Burgess JL, Chaudhari AM, Darcy MG, Donatelli CA, Luengo JI, Newlander KA, Parrish CA, Ridgers LH, Sarpong MA, Schmidt SJ, Van Aller GS, Carson JD, Diamond MA, Elkins PA, Gardiner CM, Garver E, Gilbert SA, Gontarek RR, Jackson JR, Kershner KL, Luo L, Raha K, Sherk CS, Sung CM, Sutton D, Tummino PJ, Wegrzyn RJ, Auger KR, Dhanak D. Knight SD, et al. Among authors: raha k. ACS Med Chem Lett. 2010 Jan 19;1(1):39-43. doi: 10.1021/ml900028r. eCollection 2010 Apr 8. ACS Med Chem Lett. 2010. PMID: 24900173 Free PMC article.
Discovery of a Potent Class of PI3Kα Inhibitors with Unique Binding Mode via Encoded Library Technology (ELT).
Yang H, Medeiros PF, Raha K, Elkins P, Lind KE, Lehr R, Adams ND, Burgess JL, Schmidt SJ, Knight SD, Auger KR, Schaber MD, Franklin GJ, Ding Y, DeLorey JL, Centrella PA, Mataruse S, Skinner SR, Clark MA, Cuozzo JW, Evindar G. Yang H, et al. Among authors: raha k. ACS Med Chem Lett. 2015 Mar 20;6(5):531-6. doi: 10.1021/acsmedchemlett.5b00025. eCollection 2015 May 14. ACS Med Chem Lett. 2015. PMID: 26005528 Free PMC article.
Discovery of a First-in-Class Gut-Restricted RET Kinase Inhibitor as a Clinical Candidate for the Treatment of IBS.
Schenck Eidam H, Russell J, Raha K, DeMartino M, Qin D, Guan HA, Zhang Z, Zhen G, Yu H, Wu C, Pan Y, Joberty G, Zinn N, Laquerre S, Robinson S, White A, Giddings A, Mohammadi E, Greenwood-Van Meerveld B, Oliff A, Kumar S, Cheung M. Schenck Eidam H, et al. Among authors: raha k. ACS Med Chem Lett. 2018 May 24;9(7):623-628. doi: 10.1021/acsmedchemlett.8b00035. eCollection 2018 Jul 12. ACS Med Chem Lett. 2018. PMID: 30034590 Free PMC article.
30 results