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Page 1
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
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
Respiratory syncytial virus fusion inhibitors. Part 5: Optimization of benzimidazole substitution patterns towards derivatives with improved activity.
Wang XA, Cianci CW, Yu KL, Combrink KD, Thuring JW, Zhang Y, Civiello RL, Kadow KF, Roach J, Li Z, Langley DR, Krystal M, Meanwell NA. Wang XA, et al. Among authors: langley dr. Bioorg Med Chem Lett. 2007 Aug 15;17(16):4592-8. doi: 10.1016/j.bmcl.2007.05.102. Epub 2007 Jun 8. Bioorg Med Chem Lett. 2007. PMID: 17576060
Respiratory syncytial virus fusion inhibitors. Part 6: an examination of the effect of structural variation of the benzimidazol-2-one heterocycle moiety.
Combrink KD, Gulgeze HB, Thuring JW, Yu KL, Civiello RL, Zhang Y, Pearce BC, Yin Z, Langley DR, Kadow KF, Cianci CW, Li Z, Clarke J, Genovesi EV, Medina I, Lamb L, Yang Z, Zadjura L, Krystal M, Meanwell NA. Combrink KD, et al. Among authors: langley dr. Bioorg Med Chem Lett. 2007 Sep 1;17(17):4784-90. doi: 10.1016/j.bmcl.2007.06.065. Epub 2007 Jun 26. Bioorg Med Chem Lett. 2007. PMID: 17616396
Inhibition of influenza virus replication via small molecules that induce the formation of higher-order nucleoprotein oligomers.
Gerritz SW, Cianci C, Kim S, Pearce BC, Deminie C, Discotto L, McAuliffe B, Minassian BF, Shi S, Zhu S, Zhai W, Pendri A, Li G, Poss MA, Edavettal S, McDonnell PA, Lewis HA, Maskos K, Mörtl M, Kiefersauer R, Steinbacher S, Baldwin ET, Metzler W, Bryson J, Healy MD, Philip T, Zoeckler M, Schartman R, Sinz M, Leyva-Grado VH, Hoffmann HH, Langley DR, Meanwell NA, Krystal M. Gerritz SW, et al. Among authors: langley dr. Proc Natl Acad Sci U S A. 2011 Sep 13;108(37):15366-71. doi: 10.1073/pnas.1107906108. Epub 2011 Sep 6. Proc Natl Acad Sci U S A. 2011. PMID: 21896751 Free PMC article.
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
70 results