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Page 1
Discovery of an oral respiratory syncytial virus (RSV) fusion inhibitor (GS-5806) and clinical proof of concept in a human RSV challenge study.
Mackman RL, Sangi M, Sperandio D, Parrish JP, Eisenberg E, Perron M, Hui H, Zhang L, Siegel D, Yang H, Saunders O, Boojamra C, Lee G, Samuel D, Babaoglu K, Carey A, Gilbert BE, Piedra PA, Strickley R, Iwata Q, Hayes J, Stray K, Kinkade A, Theodore D, Jordan R, Desai M, Cihlar T. Mackman RL, et al. Among authors: sperandio d. J Med Chem. 2015 Feb 26;58(4):1630-43. doi: 10.1021/jm5017768. Epub 2015 Jan 27. J Med Chem. 2015. PMID: 25574686 Clinical Trial.
Novel, potent, selective, and orally bioavailable human betaII-tryptase inhibitors.
Sperandio D, Tai VW, Lohman J, Hirschbein B, Mendonca R, Lee CS, Spencer JR, Janc J, Nguyen M, Beltman J, Sprengeler P, Scheerens H, Lin T, Liu L, Gadre A, Kellogg A, Green MJ, McGrath ME. Sperandio D, et al. Bioorg Med Chem Lett. 2006 Aug 1;16(15):4085-9. doi: 10.1016/j.bmcl.2006.04.088. Epub 2006 May 24. Bioorg Med Chem Lett. 2006. PMID: 16725321
Design, synthesis, and anti-HIV activity of 4'-modified carbocyclic nucleoside phosphonate reverse transcriptase inhibitors.
Boojamra CG, Parrish JP, Sperandio D, Gao Y, Petrakovsky OV, Lee SK, Markevitch DY, Vela JE, Laflamme G, Chen JM, Ray AS, Barron AC, Sparacino ML, Desai MC, Kim CU, Cihlar T, Mackman RL. Boojamra CG, et al. Among authors: sperandio d. Bioorg Med Chem. 2009 Feb 15;17(4):1739-46. doi: 10.1016/j.bmc.2008.12.028. Epub 2008 Dec 24. Bioorg Med Chem. 2009. PMID: 19179082
Discovery of a Potent and Orally Bioavailable Cyclophilin Inhibitor Derived from the Sanglifehrin Macrocycle.
Mackman RL, Steadman VA, Dean DK, Jansa P, Poullennec KG, Appleby T, Austin C, Blakemore CA, Cai R, Cannizzaro C, Chin G, Chiva JC, Dunbar NA, Fliri H, Highton AJ, Hui H, Ji M, Jin H, Karki K, Keats AJ, Lazarides L, Lee YJ, Liclican A, Mish M, Murray B, Pettit SB, Pyun P, Sangi M, Santos R, Sanvoisin J, Schmitz U, Schrier A, Siegel D, Sperandio D, Stepan G, Tian Y, Watt GM, Yang H, Schultz BE. Mackman RL, et al. Among authors: sperandio d. J Med Chem. 2018 Nov 8;61(21):9473-9499. doi: 10.1021/acs.jmedchem.8b00802. Epub 2018 Aug 22. J Med Chem. 2018. PMID: 30074795
Structure-guided discovery of a novel, potent, and orally bioavailable 3,5-dimethylisoxazole aryl-benzimidazole BET bromodomain inhibitor.
Sperandio D, Aktoudianakis V, Babaoglu K, Chen X, Elbel K, Chin G, Corkey B, Du J, Jiang B, Kobayashi T, Mackman R, Martinez R, Yang H, Zablocki J, Kusam S, Jordan K, Webb H, Bates JG, Lad L, Mish M, Niedziela-Majka A, Metobo S, Sapre A, Hung M, Jin D, Fung W, Kan E, Eisenberg G, Larson N, Newby ZER, Lansdon E, Tay C, Neve RM, Shevick SL, Breckenridge DG. Sperandio D, et al. Bioorg Med Chem. 2019 Feb 1;27(3):457-469. doi: 10.1016/j.bmc.2018.11.020. Epub 2018 Nov 15. Bioorg Med Chem. 2019. PMID: 30606676
Highly potent non-peptidic inhibitors of the HCV NS3/NS4A serine protease.
Sperandio D, Gangloff AR, Litvak J, Goldsmith R, Hataye JM, Wang VR, Shelton EJ, Elrod K, Janc JW, Clark JM, Rice K, Weinheimer S, Yeung KS, Meanwell NA, Hernandez D, Staab AJ, Venables BL, Spencer JR. Sperandio D, et al. Bioorg Med Chem Lett. 2002 Nov 4;12(21):3129-33. doi: 10.1016/s0960-894x(02)00680-7. Bioorg Med Chem Lett. 2002. PMID: 12372517
Discovery and structure-activity relationship of 2-phenyl-oxazole-4-carboxamide derivatives as potent apoptosis inducers.
Tai VW, Sperandio D, Shelton EJ, Litvak J, Pararajasingham K, Cebon B, Lohman J, Eksterowicz J, Kantak S, Sabbatini P, Brown C, Zeitz J, Reed C, Maske B, Graupe D, Estevez A, Oeh J, Wong D, Ni Y, Sprengeler P, Yee R, Magill C, Neri A, Cai SX, Drewe J, Qiu L, Herich J, Tseng B, Kasibhatla S, Spencer JR. Tai VW, et al. Among authors: sperandio d. Bioorg Med Chem Lett. 2006 Sep 1;16(17):4554-8. doi: 10.1016/j.bmcl.2006.06.018. Epub 2006 Jun 19. Bioorg Med Chem Lett. 2006. PMID: 16784854
Discovery of 5-(4-hydroxy-6-methyl-2-oxo-2H-pyran-3-yl)-7-phenyl-(E)-2,3,6,7-tetrahydro-1,4-thiazepines as a new series of apoptosis inducers using a cell- and caspase-based HTS assay.
Drewe J, Kasibhatla S, Tseng B, Shelton E, Sperandio D, Yee RM, Litvak J, Sendzik M, Spencer JR, Cai SX. Drewe J, et al. Among authors: sperandio d. Bioorg Med Chem Lett. 2007 Sep 1;17(17):4987-90. doi: 10.1016/j.bmcl.2007.05.098. Epub 2007 Jun 6. Bioorg Med Chem Lett. 2007. PMID: 17562361
28 results