A Review on Poly (ADP-ribose) Polymerase (PARP) Inhibitors and Synthetic Methodologies
Abstract::
Poly (ADP-ribose) polymerase (PARP) acts as an essential DNA repair enzyme.
PARP inhibitors are novel small molecule targeted drugs based on the principle of "Synthetic
Lethality", which affect DNA repair process by competitively inhibiting the activity of PARP
enzyme and thereby kill cancer cells. Currently, four PARP inhibitors including olaparib, rucaparib,
niraparib, and talazoparib have been approved by FDA for cancer treatment and have
achieved great success in the treatment of ovarian cancer, breast cancer, and pancreatic cancer,
etc. This paper provides a general overview of the research progress of PARP inhibitors
including the major structure types, structure-activity relationship (SAR), and synthetic
routes, with the aim of providing ideas for the discovery and synthesis of novel PARP inhibitors.
