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Discovery of an Atropisomeric PI3Kβ Selective Inhibitor through Optimization of the Hinge Binding Motif.
Perreault S, Arjmand F, Chandrasekhar J, Hao J, Keegan KS, Koditek D, Lepist EI, Matson CK, McGrath ME, Patel L, Sedillo K, Therrien J, Till NA, Tomkinson A, Treiberg J, Zherebina Y, Phillips G. Perreault S, et al. Among authors: patel l. ACS Med Chem Lett. 2020 Apr 13;11(6):1236-1243. doi: 10.1021/acsmedchemlett.0c00095. eCollection 2020 Jun 11. ACS Med Chem Lett. 2020. PMID: 32551006 Free PMC article.
Discovery of Orally Efficacious Phosphoinositide 3-Kinase δ Inhibitors with Improved Metabolic Stability.
Patel L, Chandrasekhar J, Evarts J, Forseth K, Haran AC, Ip C, Kashishian A, Kim M, Koditek D, Koppenol S, Lad L, Lepist EI, McGrath ME, Perreault S, Puri KD, Villaseñor AG, Somoza JR, Steiner BH, Therrien J, Treiberg J, Phillips G. Patel L, et al. J Med Chem. 2016 Oct 13;59(19):9228-9242. doi: 10.1021/acs.jmedchem.6b01169. Epub 2016 Oct 3. J Med Chem. 2016. PMID: 27660855
Discovery of a Phosphoinositide 3-Kinase (PI3K) β/δ Inhibitor for the Treatment of Phosphatase and Tensin Homolog (PTEN) Deficient Tumors: Building PI3Kβ Potency in a PI3Kδ-Selective Template by Targeting Nonconserved Asp856.
Perreault S, Chandrasekhar J, Cui ZH, Evarts J, Hao J, Kaplan JA, Kashishian A, Keegan KS, Kenney T, Koditek D, Lad L, Lepist EI, McGrath ME, Patel L, Phillips B, Therrien J, Treiberg J, Yahiaoui A, Phillips G. Perreault S, et al. Among authors: patel l. J Med Chem. 2017 Feb 23;60(4):1555-1567. doi: 10.1021/acs.jmedchem.6b01821. Epub 2017 Feb 7. J Med Chem. 2017. PMID: 28106991
Atropisomerism by Design: Discovery of a Selective and Stable Phosphoinositide 3-Kinase (PI3K) β Inhibitor.
Chandrasekhar J, Dick R, Van Veldhuizen J, Koditek D, Lepist EI, McGrath ME, Patel L, Phillips G, Sedillo K, Somoza JR, Therrien J, Till NA, Treiberg J, Villaseñor AG, Zherebina Y, Perreault S. Chandrasekhar J, et al. Among authors: patel l. J Med Chem. 2018 Aug 9;61(15):6858-6868. doi: 10.1021/acs.jmedchem.8b00797. Epub 2018 Jul 30. J Med Chem. 2018. PMID: 30015489
2,4,6-Triaminopyrimidine as a Novel Hinge Binder in a Series of PI3Kδ Selective Inhibitors.
Patel L, Chandrasekhar J, Evarts J, Haran AC, Ip C, Kaplan JA, Kim M, Koditek D, Lad L, Lepist EI, McGrath ME, Novikov N, Perreault S, Puri KD, Somoza JR, Steiner BH, Stevens KL, Therrien J, Treiberg J, Villaseñor AG, Yeung A, Phillips G. Patel L, et al. J Med Chem. 2016 Apr 14;59(7):3532-48. doi: 10.1021/acs.jmedchem.6b00213. Epub 2016 Mar 29. J Med Chem. 2016. PMID: 26980109
Discovery of (R)-6-cyclopentyl-6-(2-(2,6-diethylpyridin-4-yl)ethyl)-3-((5,7-dimethyl-[1,2,4]triazolo[1,5-a]pyrimidin-2-yl)methyl)-4-hydroxy-5,6-dihydropyran-2-one (PF-00868554) as a potent and orally available hepatitis C virus polymerase inhibitor.
Li H, Tatlock J, Linton A, Gonzalez J, Jewell T, Patel L, Ludlum S, Drowns M, Rahavendran SV, Skor H, Hunter R, Shi ST, Herlihy KJ, Parge H, Hickey M, Yu X, Chau F, Nonomiya J, Lewis C. Li H, et al. Among authors: patel l. J Med Chem. 2009 Mar 12;52(5):1255-8. doi: 10.1021/jm8014537. J Med Chem. 2009. PMID: 19209845
651 results