BIOTEKNOLOGI n sis and Evaluation of Hydrogen Peroxide Sensitive Prodrugs of Methotrexate and Aminopterin for the Treatment of Rheu- matoid Arthritis. J. Med. Chem. 2018, 61, 3503–3515. Andersen N.S.; Peiró Cadahía, J.; Pre- NH2 N N N H2N N N a OO N H OR OR O MTX, R = H R = PMB OBO O O Cl b OBO O O NH N N N H2N N N HO B OH HO B OH OO N H OPMB OPMB O c O O OH O O NH N N OH H O d N N 3 H2N N N O O NH N N N H2N N N OO N H OPMB OPMB O Skema 1. Syntese af fenylborsyre-baseret prodrug 3a a Reagenser og betingelser: (a) DIDP2E8A9,- DSkMemAaP,1CH2Cl2, 5 t (73%). PMBCl, (c) HCl 1,1,3,3-tetrametylguanidin, CH2Cl2, 16 t (35%). (b) i H2O/MeCN, 20 t (31%). (d) 5% TFA i CH2Cl2, 30 min (54%). vitali, V.; Bondebjerg, J.; Hansen, C.A.; Hansen, A.E.; Andresen, T.L.; Clausen, M.H. Methotrexate Prodrugs Sensitive to Reactive Oxygen Species for the Improved Treatment of Rheumatoid Arthritis. Eur. J. Med. Chem. 2018, in press. E-mail: Mads H. Clausen: mhc@kemi.dtu.dk Kilder 1. Smolen, J.S.; Aletaha, D.; McInnes, I.B. Rheumatoid Arthritis. Lancet 2016, 388, 2023-2038. 2. McInnes, I.B.; Schett, G. The Pathogenesis of Rheumatoid Arthritis. N. Engl. J. Med. 2011, 365, 2205-2219. 3. Huennekens, F.M. The Methotrexate Story: A Paradigm for Development of Cancer Chemotherapeutic Agents. Adv. Enzyme Regul. 1994, 34, 397-419. 4. Bannwarth, B.; Péhourcq, F.; Schaeverbeke, T.; Dehais, J. Clinical Pharmacokinetics of Low-Dose Pulse Methotrexate in Rheumatoid Arthritis. Clin. Pharmacokinet. 1996, 30, 194-210. 5. Weinblatt, M.E. Methotrexate in Rheumatoid Arthritis: A Quarter Century of Development. Trans. Am. Clin. Climatol. Assoc. 2013, 124, 16-25. 6. Stone, J.R.; Yang, S. Hydrogen Peroxide: A Signaling Messenger. Antioxid. Redox Signal. 2008, 8, 243-270. t COPENHAGEN 12. - 13. september LabDays 2018 Fagmesse for laboratorieteknik n LSB Temadag & Årsmøde n Laboratorieudstyr n Diagnostik n Bioteknologi n Forskning n Kvalitetskontrol n DSMS Temadag Øksnehallen labdays.dk - Dansk Kemi, 99, nr. 5, 2018 13
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