A Review on Poly (ADP-ribose) Polymerase (PARP) Inhibitors and Synthetic Methodologies

(E-pub Ahead of Print)

Author(s): Ying Li, Chenfu Liu, Guowu Rao*

Journal Name: Current Medicinal Chemistry

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Poly (ADP-ribose) polymerase (PARP) acts as an essential DNA repair enzyme. PARP inhibitors are a novel small molecule targeted drugs based on the principle of "Synthetic Lethality", which affect the DNA repair process by competitively inhibiting the activity of the 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.

Keywords: Ovarian cancer, Synthetic lethality, PARP inhibitors, Olaparib, Structure-activity relationship, phthalazinones, Synthesis

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(E-pub Ahead of Print)
DOI: 10.2174/0929867327666200312113011
Price: $95

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