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47 results

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Page 1
Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity.
Ndubaku CO, Heffron TP, Staben ST, Baumgardner M, Blaquiere N, Bradley E, Bull R, Do S, Dotson J, Dudley D, Edgar KA, Friedman LS, Goldsmith R, Heald RA, Kolesnikov A, Lee L, Lewis C, Nannini M, Nonomiya J, Pang J, Price S, Prior WW, Salphati L, Sideris S, Wallin JJ, Wang L, Wei B, Sampath D, Olivero AG. Ndubaku CO, et al. Among authors: staben st. J Med Chem. 2013 Jun 13;56(11):4597-610. doi: 10.1021/jm4003632. Epub 2013 Jun 3. J Med Chem. 2013. PMID: 23662903
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. 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. 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
Rational design of phosphoinositide 3-kinase α inhibitors that exhibit selectivity over the phosphoinositide 3-kinase β isoform.
Heffron TP, Wei B, Olivero A, Staben ST, Tsui V, Do S, Dotson J, Folkes AJ, Goldsmith P, Goldsmith R, Gunzner J, Lesnick J, Lewis C, Mathieu S, Nonomiya J, Shuttleworth S, Sutherlin DP, Wan NC, Wang S, Wiesmann C, Zhu BY. Heffron TP, et al. Among authors: staben st. J Med Chem. 2011 Nov 24;54(22):7815-33. doi: 10.1021/jm2007084. Epub 2011 Oct 21. J Med Chem. 2011. PMID: 21985639
Heteroarylation of azine N-oxides.
Gosselin F, Savage SJ, Blaquiere N, Staben ST. Gosselin F, et al. Among authors: staben st. Org Lett. 2012 Feb 3;14(3):862-5. doi: 10.1021/ol203388j. Epub 2012 Jan 19. Org Lett. 2012. PMID: 22260711
Potent and selective inhibitors of PI3Kδ: obtaining isoform selectivity from the affinity pocket and tryptophan shelf.
Sutherlin DP, Baker S, Bisconte A, Blaney PM, Brown A, Chan BK, Chantry D, Castanedo G, DePledge P, Goldsmith P, Goldstein DM, Hancox T, Kaur J, Knowles D, Kondru R, Lesnick J, Lucas MC, Lewis C, Murray J, Nadin AJ, Nonomiya J, Pang J, Pegg N, Price S, Reif K, Safina BS, Salphati L, Staben S, Seward EM, Shuttleworth S, Sohal S, Sweeney ZK, Ultsch M, Waszkowycz B, Wei B. Sutherlin DP, et al. Bioorg Med Chem Lett. 2012 Jul 1;22(13):4296-302. doi: 10.1016/j.bmcl.2012.05.027. Epub 2012 May 17. Bioorg Med Chem Lett. 2012. PMID: 22672799
Cis-amide isosteric replacement in thienobenzoxepin inhibitors of PI3-kinase.
Staben ST, Blaquiere N, Tsui V, Kolesnikov A, Do S, Bradley EK, Dotson J, Goldsmith R, Heffron TP, Lesnick J, Lewis C, Murray J, Nonomiya J, Olivero AG, Pang J, Rouge L, Salphati L, Wei B, Wiesmann C, Wu P. Staben ST, et al. Bioorg Med Chem Lett. 2013 Feb 1;23(3):897-901. doi: 10.1016/j.bmcl.2012.10.121. Epub 2012 Nov 5. Bioorg Med Chem Lett. 2013. PMID: 23265894
Discovery of thiazolobenzoxepin PI3-kinase inhibitors that spare the PI3-kinase β isoform.
Staben ST, Ndubaku C, Blaquiere N, Belvin M, Bull RJ, Dudley D, Edgar K, Gray D, Heald R, Heffron TP, Jones GE, Jones M, Kolesnikov A, Lee L, Lesnick J, Lewis C, Murray J, McLean NJ, Nonomiya J, Olivero AG, Ord R, Pang J, Price S, Prior WW, Rouge L, Salphati L, Sampath D, Wallin J, Wang L, Wei B, Weismann C, Wu P. Staben ST, et al. Bioorg Med Chem Lett. 2013 May 1;23(9):2606-13. doi: 10.1016/j.bmcl.2013.02.102. Epub 2013 Mar 7. Bioorg Med Chem Lett. 2013. PMID: 23540645
47 results