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The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326).
Heffron TP, Heald RA, Ndubaku C, Wei B, Augistin M, Do S, Edgar K, Eigenbrot C, Friedman L, Gancia E, Jackson PS, Jones G, Kolesnikov A, Lee LB, Lesnick JD, Lewis C, McLean N, Mörtl M, Nonomiya J, Pang J, Price S, Prior WW, Salphati L, Sideris S, Staben ST, Steinbacher S, Tsui V, Wallin J, Sampath D, Olivero AG. Heffron TP, et al. Among authors: sampath d. J Med Chem. 2016 Feb 11;59(3):985-1002. doi: 10.1021/acs.jmedchem.5b01483. Epub 2016 Jan 20. J Med Chem. 2016. PMID: 26741947
Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors for the treatment of cancer.
Sutherlin DP, Sampath D, Berry M, Castanedo G, Chang Z, Chuckowree I, Dotson J, Folkes A, Friedman L, Goldsmith R, Heffron T, Lee L, Lesnick J, Lewis C, Mathieu S, Nonomiya J, Olivero A, Pang J, Prior WW, Salphati L, Sideris S, Tian Q, Tsui V, Wan NC, Wang S, Wiesmann C, Wong S, Zhu BY. Sutherlin DP, et al. Among authors: sampath d. J Med Chem. 2010 Feb 11;53(3):1086-97. doi: 10.1021/jm901284w. J Med Chem. 2010. PMID: 20050669
Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor.
Heffron TP, Berry M, Castanedo G, Chang C, Chuckowree I, Dotson J, Folkes A, Gunzner J, Lesnick JD, Lewis C, Mathieu S, Nonomiya J, Olivero A, Pang J, Peterson D, Salphati L, Sampath D, Sideris S, Sutherlin DP, Tsui V, Wan NC, Wang S, Wong S, Zhu BY. Heffron TP, et al. Among authors: sampath d. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2408-11. doi: 10.1016/j.bmcl.2010.03.046. Epub 2010 Mar 12. Bioorg Med Chem Lett. 2010. PMID: 20346656
Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase.
Staben ST, Heffron TP, Sutherlin DP, Bhat SR, Castanedo GM, Chuckowree IS, Dotson J, Folkes AJ, Friedman LS, Lee L, Lesnick J, Lewis C, Murray JM, Nonomiya J, Olivero AG, Plise E, Pang J, Prior WW, Salphati L, Rouge L, Sampath D, Tsui V, Wan NC, Wang S, Weismann C, Wu P, Zhu BY. Staben ST, et al. Among authors: sampath d. Bioorg Med Chem Lett. 2010 Oct 15;20(20):6048-51. doi: 10.1016/j.bmcl.2010.08.067. Epub 2010 Aug 19. Bioorg Med Chem Lett. 2010. PMID: 20822905
Structure-based design of thienobenzoxepin inhibitors of PI3-kinase.
Staben ST, Siu M, Goldsmith R, Olivero AG, Do S, Burdick DJ, Heffron TP, Dotson J, Sutherlin DP, Zhu BY, Tsui V, Le H, Lee L, Lesnick J, Lewis C, Murray JM, Nonomiya J, Pang J, Prior WW, Salphati L, Rouge L, Sampath D, Sideris S, Wiesmann C, Wu P. Staben ST, et al. Among authors: sampath d. Bioorg Med Chem Lett. 2011 Jul 1;21(13):4054-8. doi: 10.1016/j.bmcl.2011.04.124. Epub 2011 May 13. Bioorg Med Chem Lett. 2011. PMID: 21636270
214 results