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Medientyp: E-Artikel Titel: Ferrocene‐modified thiopyrimidines: synthesis, enantiomeric resolution, antitumor activity Beteiligte: Simenel, Alexander A.; Dokuchaeva, Galina A.; Snegur, Lubov' V.; Rodionov, Alexey N.; Ilyin, Mikhail M.; Zykova, Svetlana I.; Ostrovskaya, Larissa A.; Bluchterova, Natalia V.; Fomina, Margarita M.; Rikova, Valentina A. Erschienen: Wiley, 2011 Erschienen in: Applied Organometallic Chemistry Sprache: Englisch DOI: 10.1002/aoc.1691 ISSN: 0268-2605; 1099-0739 Schlagwörter: Inorganic Chemistry ; General Chemistry Entstehung: Anmerkungen: Beschreibung: <jats:title>Abstract</jats:title><jats:p>Ferrocenylalkyl thiopyrimidines (<jats:bold>6a–d</jats:bold> to <jats:bold>9a–d</jats:bold>) were prepared via the reaction of the α‐(hydroxy)alkyl ferrocenes, FcCHR(OH) (<jats:bold>1a–d</jats:bold>; Fc = ferrocenyl; R = H, Me, Et, Ph), with 2‐thiopyrimidines (<jats:bold>2</jats:bold>–<jats:bold>5</jats:bold>) in acetone at room temperature in the presence of TFA, yielding 50–95%. The resulting enantiomers were resolved using HPLC on modified cellulose as chiral selector. The antitumor activities of <jats:italic>S</jats:italic>‐ferrocenylethyl 2‐thiopyrimidine (<jats:bold>6b</jats:bold>) against two murine solid tumor models, carcinoma 755 (Ca755) and Lewis lung carcinoma (LLC) were evaluated <jats:italic>in vivo</jats:italic>. The strong antitumor effect of compound <jats:bold>6b</jats:bold> on Ca755 and LLC was demonstrated. The index of tumor growth inhibition on Ca755 equaled 95% in comparison with control. Copyright © 2010 John Wiley & Sons, Ltd.</jats:p>