Abstract

REVIEW OF QUINAZOLINONE SCAFFOLD AS ANTICANCER AGENTS

Kavitha K.*, Srinivasan N. and Harbabu Y.

Abstract

Although many types of chemotherapeutic agents are currently used to treat human cancers, either in combination or alone, they have limited effectiveness, the response rates remain largely unimproved in clinical trials. Quinazolinone a class of epidermal growth factor receptor (EGFR) inhibitors which plays a vital role in cell growth regulation and considered one of the most intensely studied targets of tyrosine kinas inhibitors. Despite, chemistry of quinazolinone being as an established area, day by day newer, more complex derivatives of quinazolinone compounds are still being discovered. Moreover, an assortment of literature, quinazolinone exhibits a strong lactam-lactim tautomeric interaction and furthermore, when the methyl group is present in the position-2, the tautomeric effect is increased, including structure activity relationship studies of quinazolinone ring system states that the position -2,6 and 8, of the ring system, these positions are very much important for structure activity studies and also suggested that the inclusion of different heterocyclic moieties at position -3 of the quinazolinone ring system could be increased chemotherapeutic activity. Pharmacologically quinazolinone are the most important class of heterocyclic compounds among the quinazoline nucleus. The stability of nucleus has inspired medicinal chemists to introduce many bioactive moieties to synthesize new potential therapeutic agents. This review was based on the quinazolinone and, its derivatives exhibiting various types of cancer activities with different substituent.

Keywords: quinazolinone, EGFR, antitumor, cytotoxic activity, anti proliferative activity.