4.6 Article

Synthesis of disaccharide nucleoside analogues as potential poly(ADP-ribose) polymerase-1 inhibitors

Journal

ORGANIC & BIOMOLECULAR CHEMISTRY
Volume 16, Issue 46, Pages 8904-8907

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/c8ob01894d

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Funding

  1. Konstanz Research School Chemical Biology (KoRS-CB)
  2. DFG [SPP 1623]
  3. KoRS-CB

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Poly(ADP-ribose) polymerase-1 (PARP-1) is an important target in cancer therapy. We present the synthesis of novel disaccharide nucleoside analogues that resemble the central motif of poly(ADP-ribose) and test their inhibitory effects on human PARP-1. Some compounds show inhibition of enzymatic activity in vitro and thus might be interesting for further investigations.

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