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Discovery of new acylaminopyridines as GSK-3 inhibitors by a structure guided in-depth exploration of chemical space around a pyrrolopyridinone core.
Sivaprakasam P, Han X, Civiello RL, Jacutin-Porte S, Kish K, Pokross M, Lewis HA, Ahmed N, Szapiel N, Newitt JA, Baldwin ET, Xiao H, Krause CM, Park H, Nophsker M, Lippy JS, Burton CR, Langley DR, Macor JE, Dubowchik GM. Sivaprakasam P, et al. Among authors: langley dr. Bioorg Med Chem Lett. 2015 May 1;25(9):1856-63. doi: 10.1016/j.bmcl.2015.03.046. Epub 2015 Mar 24. Bioorg Med Chem Lett. 2015. PMID: 25845281
Discovery of Isonicotinamides as Highly Selective, Brain Penetrable, and Orally Active Glycogen Synthase Kinase-3 Inhibitors.
Luo G, Chen L, Burton CR, Xiao H, Sivaprakasam P, Krause CM, Cao Y, Liu N, Lippy J, Clarke WJ, Snow K, Raybon J, Arora V, Pokross M, Kish K, Lewis HA, Langley DR, Macor JE, Dubowchik GM. Luo G, et al. Among authors: langley dr. J Med Chem. 2016 Feb 11;59(3):1041-51. doi: 10.1021/acs.jmedchem.5b01550. Epub 2016 Jan 22. J Med Chem. 2016. PMID: 26751161
Discovery and Optimization of Novel Pyrazolopyrimidines as Potent and Orally Bioavailable Allosteric HIV-1 Integrase Inhibitors.
Li G, Meanwell NA, Krystal MR, Langley DR, Naidu BN, Sivaprakasam P, Lewis H, Kish K, Khan JA, Ng A, Trainor GL, Cianci C, Dicker IB, Walker MA, Lin Z, Protack T, Discotto L, Jenkins S, Gerritz SW, Pendri A. Li G, et al. Among authors: langley dr. J Med Chem. 2020 Mar 12;63(5):2620-2637. doi: 10.1021/acs.jmedchem.9b01681. Epub 2020 Feb 21. J Med Chem. 2020. PMID: 32081010
Design, Synthesis, and Structure-Activity Relationships of Novel Tetrahydroisoquinolino Benzodiazepine Dimer Antitumor Agents and Their Application in Antibody-Drug Conjugates.
Chowdari NS, Zhang Y, McDonald I, Johnson W, Langley DR, Sivaprakasam P, Mate R, Huynh T, Kotapati S, Deshpande M, Pan C, Menezes D, Wang Y, Rao C, Sarma G, Warrack BM, Rangan VS, Mei-Chen S, Cardarelli P, Deshpande S, Passmore D, Rampulla R, Mathur A, Borzilleri R, Rajpal A, Vite G, Gangwar S. Chowdari NS, et al. Among authors: langley dr. J Med Chem. 2020 Nov 25;63(22):13913-13950. doi: 10.1021/acs.jmedchem.0c01385. Epub 2020 Nov 6. J Med Chem. 2020. PMID: 33155811
Structure-based amelioration of PXR transactivation in a novel series of macrocyclic allosteric inhibitors of HIV-1 integrase.
Sivaprakasam P, Wang Z, Meanwell NA, Khan JA, Langley DR, Johnson SR, Li G, Pendri A, Connolly TP, Gao M, Camac DM, Klakouski C, Zvyaga T, Cianci C, McAuliffe B, Ding B, Discotto L, Krystal MR, Jenkins S, Peese KM, Narasimhulu Naidu B. Sivaprakasam P, et al. Among authors: langley dr. Bioorg Med Chem Lett. 2020 Nov 15;30(22):127531. doi: 10.1016/j.bmcl.2020.127531. Epub 2020 Sep 2. Bioorg Med Chem Lett. 2020. PMID: 32890685
Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 12. Structure-activity relationships associated with 4-fluoro-6-azaindole derivatives leading to the identification of 1-(4-benzoylpiperazin-1-yl)-2-(4-fluoro-7-[1,2,3]triazol-1-yl-1h-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-585248).
Regueiro-Ren A, Xue QM, Swidorski JJ, Gong YF, Mathew M, Parker DD, Yang Z, Eggers B, D'Arienzo C, Sun Y, Malinowski J, Gao Q, Wu D, Langley DR, Colonno RJ, Chien C, Grasela DM, Zheng M, Lin PF, Meanwell NA, Kadow JF. Regueiro-Ren A, et al. Among authors: langley dr. J Med Chem. 2013 Feb 28;56(4):1656-69. doi: 10.1021/jm3016377. Epub 2013 Feb 7. J Med Chem. 2013. PMID: 23360431
70 results