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Rational design of an AKR1C3-resistant analog of PR-104 for enzyme-prodrug therapy.
Mowday AM, Ashoorzadeh A, Williams EM, Copp JN, Silva S, Bull MR, Abbattista MR, Anderson RF, Flanagan JU, Guise CP, Ackerley DF, Smaill JB, Patterson AV. Mowday AM, et al. Among authors: silva s. Biochem Pharmacol. 2016 Sep 15;116:176-87. doi: 10.1016/j.bcp.2016.07.015. Epub 2016 Jul 22. Biochem Pharmacol. 2016. PMID: 27453434
Restoring Tumour Selectivity of the Bioreductive Prodrug PR-104 by Developing an Analogue Resistant to Aerobic Metabolism by Human Aldo-Keto Reductase 1C3.
Abbattista MR, Ashoorzadeh A, Guise CP, Mowday AM, Mittra R, Silva S, Hicks KO, Bull MR, Jackson-Patel V, Lin X, Prosser GA, Lambie NK, Dachs GU, Ackerley DF, Smaill JB, Patterson AV. Abbattista MR, et al. Among authors: silva s. Pharmaceuticals (Basel). 2021 Nov 26;14(12):1231. doi: 10.3390/ph14121231. Pharmaceuticals (Basel). 2021. PMID: 34959631 Free PMC article.
3-(3,4-Dihydroisoquinolin-2(1H)-ylsulfonyl)benzoic Acids: highly potent and selective inhibitors of the type 5 17-β-hydroxysteroid dehydrogenase AKR1C3.
Jamieson SM, Brooke DG, Heinrich D, Atwell GJ, Silva S, Hamilton EJ, Turnbull AP, Rigoreau LJ, Trivier E, Soudy C, Samlal SS, Owen PJ, Schroeder E, Raynham T, Flanagan JU, Denny WA. Jamieson SM, et al. Among authors: silva s. J Med Chem. 2012 Sep 13;55(17):7746-58. doi: 10.1021/jm3007867. Epub 2012 Aug 21. J Med Chem. 2012. PMID: 22877157
Synthesis and structure-activity relationships for 1-(4-(piperidin-1-ylsulfonyl)phenyl)pyrrolidin-2-ones as novel non-carboxylate inhibitors of the aldo-keto reductase enzyme AKR1C3.
Heinrich DM, Flanagan JU, Jamieson SM, Silva S, Rigoreau LJ, Trivier E, Raynham T, Turnbull AP, Denny WA. Heinrich DM, et al. Among authors: silva s. Eur J Med Chem. 2013 Apr;62:738-44. doi: 10.1016/j.ejmech.2013.01.047. Epub 2013 Feb 9. Eur J Med Chem. 2013. PMID: 23454516
5,723 results