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Page 1
Identification and Optimization of a Series of 8-Hydroxy Naphthyridines with Potent In Vitro Antileishmanial Activity: Initial SAR and Assessment of In Vivo Activity.
Thomas MG, De Rycker M, Wall RJ, Spinks D, Epemolu O, Manthri S, Norval S, Osuna-Cabello M, Patterson S, Riley J, Simeons FRC, Stojanovski L, Thomas J, Thompson S, Naylor C, Fiandor JM, Wyatt PG, Marco M, Wyllie S, Read KD, Miles TJ, Gilbert IH. Thomas MG, et al. Among authors: epemolu o. J Med Chem. 2020 Sep 10;63(17):9523-9539. doi: 10.1021/acs.jmedchem.0c00705. Epub 2020 Aug 13. J Med Chem. 2020. PMID: 32663005 Free PMC article.
The discovery and SAR of indoline-3-carboxamides--a new series of 5-HT6 antagonists.
Reid M, Carlyle I, Caulfield WL, Clarkson TR, Cusick F, Epemolu O, Gilfillan R, Goodwin R, Jaap D, O'Donnell EC, Presland J, Rankovic Z, Spinks D, Spinks G, Thomson AM, Thomson F, Strain J, Wishart G. Reid M, et al. Among authors: o donnell ec, epemolu o. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3713-6. doi: 10.1016/j.bmcl.2010.04.085. Epub 2010 Apr 24. Bioorg Med Chem Lett. 2010. PMID: 20471831
Essential but Not Vulnerable: Indazole Sulfonamides Targeting Inosine Monophosphate Dehydrogenase as Potential Leads against Mycobacterium tuberculosis.
Park Y, Pacitto A, Bayliss T, Cleghorn LA, Wang Z, Hartman T, Arora K, Ioerger TR, Sacchettini J, Rizzi M, Donini S, Blundell TL, Ascher DB, Rhee K, Breda A, Zhou N, Dartois V, Jonnala SR, Via LE, Mizrahi V, Epemolu O, Stojanovski L, Simeons F, Osuna-Cabello M, Ellis L, MacKenzie CJ, Smith AR, Davis SH, Murugesan D, Buchanan KI, Turner PA, Huggett M, Zuccotto F, Rebollo-Lopez MJ, Lafuente-Monasterio MJ, Sanz O, Diaz GS, Lelièvre J, Ballell L, Selenski C, Axtman M, Ghidelli-Disse S, Pflaumer H, Bösche M, Drewes G, Freiberg GM, Kurnick MD, Srikumaran M, Kempf DJ, Green SR, Ray PC, Read K, Wyatt P, Barry CE 3rd, Boshoff HI. Park Y, et al. Among authors: epemolu o. ACS Infect Dis. 2017 Jan 13;3(1):18-33. doi: 10.1021/acsinfecdis.6b00103. Epub 2016 Oct 17. ACS Infect Dis. 2017. PMID: 27704782 Free PMC article.
Development of a Novel Lead that Targets M. tuberculosis Polyketide Synthase 13.
Aggarwal A, Parai MK, Shetty N, Wallis D, Woolhiser L, Hastings C, Dutta NK, Galaviz S, Dhakal RC, Shrestha R, Wakabayashi S, Walpole C, Matthews D, Floyd D, Scullion P, Riley J, Epemolu O, Norval S, Snavely T, Robertson GT, Rubin EJ, Ioerger TR, Sirgel FA, van der Merwe R, van Helden PD, Keller P, Böttger EC, Karakousis PC, Lenaerts AJ, Sacchettini JC. Aggarwal A, et al. Among authors: epemolu o. Cell. 2017 Jul 13;170(2):249-259.e25. doi: 10.1016/j.cell.2017.06.025. Epub 2017 Jun 29. Cell. 2017. PMID: 28669536 Free PMC article.
Discovery and Optimization of 5-Amino-1,2,3-triazole-4-carboxamide Series against Trypanosoma cruzi.
Brand S, Ko EJ, Viayna E, Thompson S, Spinks D, Thomas M, Sandberg L, Francisco AF, Jayawardhana S, Smith VC, Jansen C, De Rycker M, Thomas J, MacLean L, Osuna-Cabello M, Riley J, Scullion P, Stojanovski L, Simeons FRC, Epemolu O, Shishikura Y, Crouch SD, Bakshi TS, Nixon CJ, Reid IH, Hill AP, Underwood TZ, Hindley SJ, Robinson SA, Kelly JM, Fiandor JM, Wyatt PG, Marco M, Miles TJ, Read KD, Gilbert IH. Brand S, et al. Among authors: epemolu o. J Med Chem. 2017 Sep 14;60(17):7284-7299. doi: 10.1021/acs.jmedchem.7b00463. Epub 2017 Aug 27. J Med Chem. 2017. PMID: 28844141 Free PMC article.
Group-Based Optimization of Potent and Cell-Active Inhibitors of the von Hippel-Lindau (VHL) E3 Ubiquitin Ligase: Structure-Activity Relationships Leading to the Chemical Probe (2S,4R)-1-((S)-2-(1-Cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (VH298).
Soares P, Gadd MS, Frost J, Galdeano C, Ellis L, Epemolu O, Rocha S, Read KD, Ciulli A. Soares P, et al. Among authors: epemolu o. J Med Chem. 2018 Jan 25;61(2):599-618. doi: 10.1021/acs.jmedchem.7b00675. Epub 2017 Sep 18. J Med Chem. 2018. PMID: 28853884 Free PMC article.
Chemical Validation of Methionyl-tRNA Synthetase as a Druggable Target in Leishmania donovani.
Torrie LS, Brand S, Robinson DA, Ko EJ, Stojanovski L, Simeons FRC, Wyllie S, Thomas J, Ellis L, Osuna-Cabello M, Epemolu O, Nühs A, Riley J, MacLean L, Manthri S, Read KD, Gilbert IH, Fairlamb AH, De Rycker M. Torrie LS, et al. Among authors: epemolu o. ACS Infect Dis. 2017 Oct 13;3(10):718-727. doi: 10.1021/acsinfecdis.7b00047. Epub 2017 Oct 2. ACS Infect Dis. 2017. PMID: 28967262 Free PMC article.
2-Mercapto-Quinazolinones as Inhibitors of Type II NADH Dehydrogenase and Mycobacterium tuberculosis: Structure-Activity Relationships, Mechanism of Action and Absorption, Distribution, Metabolism, and Excretion Characterization.
Murugesan D, Ray PC, Bayliss T, Prosser GA, Harrison JR, Green K, Soares de Melo C, Feng TS, Street LJ, Chibale K, Warner DF, Mizrahi V, Epemolu O, Scullion P, Ellis L, Riley J, Shishikura Y, Ferguson L, Osuna-Cabello M, Read KD, Green SR, Lamprecht DA, Finin PM, Steyn AJC, Ioerger TR, Sacchettini J, Rhee KY, Arora K, Barry CE 3rd, Wyatt PG, Boshoff HIM. Murugesan D, et al. Among authors: epemolu o. ACS Infect Dis. 2018 Jun 8;4(6):954-969. doi: 10.1021/acsinfecdis.7b00275. Epub 2018 Mar 26. ACS Infect Dis. 2018. PMID: 29522317 Free PMC article.
39 results