title: Inhibition of poly(adenosine diphosphate-ribose) polymerase using quinazolinone nucleus.
abstract: Poly(adenosine diphosphate-ribose) polymerase (PARP) is a group of enzymes with several subtypes and it manages various ailment such as cancer, inflammatory disorders, diabetes mellitus, neuronal injury, HIV infection, Parkinsonism, aging, and ischemia-reperfusion injury. Various PARP inhibitors share a common property of bicyclic lactam in its main structural frame. The core moiety containing bicyclic lactam rings are isoquinolinones, dihydroisoquinolinones, quinazolinediones, phthalazinones, quinazolinones, and phenanthridones. The quinazolinone with diverse substituents displayed low nanomolar inhibition. Quinazolinone is an important and vital molecule in the field of medicinal chemistry possessing multitude pharmacological actions. Though the chemistry of quinazolinones has been discussed through centuries, its concise role on PARP inhibition needed a special consideration. The aim of this review is to discover the effect of quinazolinone substitutents and its role in PARP inhibition. This precise review will discuss the effect of quinazolinones on PARP subtypes such as PARP-1, PARP-2, PARP-5a, and PARP-5b. In addition to its pharmacological actions, PARP inhibitors can also act as a chemosensitizing agent, and it is used in combination with the other anticancer agents. This summarization will definitely be a supportive report for the scientist working toward the novelty in the quinazolinone nucleus and its role in PARP inhibition.
authors.affiliation: Chemistry of Heterocycles & Natural Product Research Laboratory, Department of Chemistry, School of Advanced Sciences, VIT University, Vellore, Tamil Nadu, 632 014, India.
authors.forename: K
authors.initials: K
authors.lastname: Hemalatha
authors.affiliation: Chemistry of Heterocycles & Natural Product Research Laboratory, Department of Chemistry, School of Advanced Sciences, VIT University, Vellore, Tamil Nadu, 632 014, India. dr.g.madhumitha@gmail.com.
authors.forename: G
authors.initials: G
authors.lastname: Madhumitha
mesh_terms: D000067856:Poly(ADP-ribose) Polymerase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D011065:Poly(ADP-ribose) Polymerases / Q000378:metabolism*; D052999:Quinazolinones / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000067856:Poly(ADP-ribose) Polymerase Inhibitors; D052999:Quinazolinones; D011065:Poly(ADP-ribose) Polymerases
keywords: Bicyclic lactams; Chemosensitizing agent; PARP inhibitors; PARP subtypes; Quinazolinone