2. Academic Validation
  3. New 3'-O-aromatic acyl-5-fluoro-2'-deoxyuridine derivatives as potential anticancer agents

New 3'-O-aromatic acyl-5-fluoro-2'-deoxyuridine derivatives as potential anticancer agents

  • Eur J Med Chem. 2016 Jun 10:115:41-52. doi: 10.1016/j.ejmech.2016.03.010.
Agnieszka Szymańska-Michalak 1,  Dariusz Wawrzyniak 1,  Grzegorz Framski 1,  Marta Kujda 2,  Paulina Zgoła 1,  Jacek Stawinski 1,  Jan Barciszewski 1,  Jerzy Boryski 1,  Adam Kraszewski 3
Affiliations

Affiliations

  • 1 Institute of Bioorganic Chemistry, Polish Academy of Sciences, Noskowskiego 12/14, 61-704, Poznań, Poland.
  • 2 Jerzy Haber Institute of Catalysis and Surface Chemistry, Polish Academy of Sciences, Niezapominajek 8, 30-239, Cracow, Poland.
  • 3 Institute of Bioorganic Chemistry, Polish Academy of Sciences, Noskowskiego 12/14, 61-704, Poznań, Poland. Electronic address: [email protected].
PMID: 26994842 DOI: 10.1016/j.ejmech.2016.03.010
Abstract

New aromatic and aliphatic 3'-O-acyl-5-fluoro-2'-deoxyuridine derivatives were synthesized and evaluated as candidates for prodrugs against various Cancer cell lines. As the most promising candidate for antimalignant therapeutics was found a dual-acting acyl derivative 7h, which apparently released not only the known Anticancer nucleoside, 5-fluoro-2'-deoxyuridine (FdU), but also an additional active metabolite, acetylsalicylic acid, reinforcing thus therapeutic effect of FdU. Promising therapeutic indices showed also some aromatic dicarboxylic acids derivatives decorated with FdU esters (11 and 12).

Keywords

5-fluoro-2′-deoxyuridine; Anticancer; Double barrelled; Glioblastoma multiforme; Multi decorated; Nucleoside analogues.

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