4-Phenyl-1,2,3,6-tetrahydropyridine, an excellent fragment to improve the potency of PARP-1 inhibitors

Bioorg Med Chem Lett. 2005 Oct 1;15(19):4221-5. doi: 10.1016/j.bmcl.2005.06.094.


We have shown that a 4-phenyl-1,2,3,6-tetrahydropyridine fragment plays an important role in improving inhibitory potency against poly(ADP-ribose) polymerase-1 (PARP-1). Various benzamide analogues linked with this fragment via alkyl spacers have been prepared and evaluated. As a result, some of them have been found to be highly potent PARP-1 inhibitors.

MeSH terms

  • 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine / analogs & derivatives*
  • 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine / chemical synthesis
  • 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine / pharmacology
  • Antipyrine
  • Benzamides
  • Humans
  • Inhibitory Concentration 50
  • Poly (ADP-Ribose) Polymerase-1
  • Poly(ADP-ribose) Polymerase Inhibitors*
  • Structure-Activity Relationship


  • Benzamides
  • Poly(ADP-ribose) Polymerase Inhibitors
  • 4-phenyl-1,2,3,6-tetrahydropyridine
  • 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine
  • PARP1 protein, human
  • Poly (ADP-Ribose) Polymerase-1
  • Antipyrine