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799 results

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Page 1
Filling a nick in NIK: Extending the half-life of a NIK inhibitor through structure-based drug design.
Crawford JJ, Feng J, Brightbill HD, Johnson AR, Wright M, Kolesnikov A, Lee W, Castanedo GM, Do S, Blaquiere N, Staben ST, Chiang PC, Fan PW, Baumgardner M, Wong S, Godemann R, Grabbe A, Wiegel C, Sujatha-Bhaskar S, Hymowitz SG, Liau N, Hsu PL, McEwan PA, Ismaili MHA, Landry ML. Crawford JJ, et al. Among authors: do s. Bioorg Med Chem Lett. 2023 Jun 1;89:129277. doi: 10.1016/j.bmcl.2023.129277. Epub 2023 Apr 25. Bioorg Med Chem Lett. 2023. PMID: 37105490
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: do s. 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: do s. J Med Chem. 2011 Nov 24;54(22):7815-33. doi: 10.1021/jm2007084. Epub 2011 Oct 21. J Med Chem. 2011. PMID: 21985639
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. Among authors: do s. 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 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: do s. J Med Chem. 2013 Jun 13;56(11):4597-610. doi: 10.1021/jm4003632. Epub 2013 Jun 3. J Med Chem. 2013. PMID: 23662903
Discovery of 3,5-substituted 6-azaindazoles as potent pan-Pim inhibitors.
Hu H, Wang X, Chan GK, Chang JH, Do S, Drummond J, Ebens A, Lee W, Ly J, Lyssikatos JP, Murray J, Moffat JG, Chao Q, Tsui V, Wallweber H, Kolesnikov A. Hu H, et al. Among authors: do s. Bioorg Med Chem Lett. 2015 Nov 15;25(22):5258-64. doi: 10.1016/j.bmcl.2015.09.052. Epub 2015 Sep 30. Bioorg Med Chem Lett. 2015. PMID: 26459208
α-Aryl pyrrolidine sulfonamides as TRPA1 antagonists.
Verma VA, Shore DGM, Chen H, Chen J, Do S, Hackos DH, Kolesnikov A, Lyssikatos JP, Tay S, Wang L, Estrada AA. Verma VA, et al. Among authors: do s. Bioorg Med Chem Lett. 2016 Jan 15;26(2):495-498. doi: 10.1016/j.bmcl.2015.11.088. Epub 2015 Nov 25. Bioorg Med Chem Lett. 2016. PMID: 26706172
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: do s. 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 a Potent (4 R,5 S)-4-Fluoro-5-methylproline Sulfonamide Transient Receptor Potential Ankyrin 1 Antagonist and Its Methylene Phosphate Prodrug Guided by Molecular Modeling.
Chen H, Volgraf M, Do S, Kolesnikov A, Shore DG, Verma VA, Villemure E, Wang L, Chen Y, Hu B, Lu AJ, Wu G, Xu X, Yuen PW, Zhang Y, Erickson SD, Dahl M, Brotherton-Pleiss C, Tay S, Ly JQ, Murray LJ, Chen J, Amm D, Lange W, Hackos DH, Reese RM, Shields SD, Lyssikatos JP, Safina BS, Estrada AA. Chen H, et al. Among authors: do s. J Med Chem. 2018 Apr 26;61(8):3641-3659. doi: 10.1021/acs.jmedchem.8b00117. Epub 2018 Apr 12. J Med Chem. 2018. PMID: 29590749
799 results