Design, synthesis and biological activity of novel molecules designed to target PARP and DNA

[Display omitted] In order to enhance the cytotoxic potential of poly(ADP-ribose) polymerase (PARP) inhibitors in BRCA1 or 2 deficient tumours, we designed a series of molecules containing a 1,2,3-triazene moiety tethered to a PARP targeting scaffold. A cell-based selectivity assay involving a BRCA2...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2017-02, Vol.27 (3), p.688-694
Hauptverfasser:	Goodfellow, Elliot, Senhaji Mouhri, Zhor, Williams, Christopher, Jean-Claude, Bertrand J.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Binding Sites Bis-targeting BRCA mutation BRCA2 Protein - deficiency BRCA2 Protein - genetics CHO Cells Cricetinae Cricetulus DNA - chemistry DNA - metabolism DNA damage DNA Damage - drug effects Drug Design Enzyme Activation - drug effects Molecular Docking Simulation PARP inhibitors Poly(ADP-ribose) Polymerase Inhibitors - chemical synthesis Poly(ADP-ribose) Polymerase Inhibitors - chemistry Poly(ADP-ribose) Polymerase Inhibitors - pharmacology Poly(ADP-ribose) Polymerases - chemistry Poly(ADP-ribose) Polymerases - metabolism Protein Structure, Tertiary Synthetic lethality
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