Title:Bestowal of Quinazoline Scaffold in Anticancer Drug Discovery
Volume: 21
Issue: 11
Author(s): Rina Das, Dinesh K. Mehta and Meenakshi Dhanawat*
Affiliation:
- MM College of Pharmacy, MM (Deemed to be University), Mullana, Ambala, HR, 133207,India
Keywords:
Quinazoline, anticancer, EGFR, thymidylate enzyme, DNA inhibition, tubulin polymerization.
Abstract:
Background: Cancer is one of the major causes of human mortality worldwide. A number of existing
antineoplastic medications and treatment regimens are already working in the field, and several new compounds
are in different phases of clinical trials. An extensive series of anticancer drugs exist in the market, and studies
suggest that these molecules are associated with different types of adverse side effects. The reduction of the
cytotoxicity of drugs to normal cells is a major problem in anticancer therapy.
Therefore, researchers around the globe are involved in the development of more efficient and safer anticancer
drugs. The output of extensive research is that the quinazoline scaffold and its various derivatives can be explored
further as a novel class of cancer chemotherapeutic agents that has already shown promising activities
against different tumours. Quinazoline derivatives have already occupied a crucial place in modern medicinal
chemistry. Various research has been performed on quinazoline and their derivatives for anticancer activity and
pharmacological importance of this scaffold has been well established.
Objective: The aim of this review is to compile and highlight the developments concerning the anticancer activity
of quinazoline derivatives as well as to suggest some new aspects of the expansion of anticancer activity of
novel quinazoline derivatives as anticancer agents in the near future.
Methods: Recent literature related to quinazoline derivatives endowed with encouraging anticancer potential is
reviewed. With a special focus on quinazoline moiety, this review offers a detailed account of multiple mechanisms
of action of various quinazoline derivatives: inhibition of the DNA repair enzyme system, inhibition of
EGFR, thymidylate enzyme inhibition and inhibitory effects for tubulin polymerization by which these derivatives
have shown promising anticancer potential.
Results: Exhaustive literature survey indicated that quinazoline derivatives are associated with properties of
inhibiting EGFR and thymidylate enzymes. It was also found to be involved in disturbing tubulin assembly.
Furthermore, quinazoline derivatives have been found to inhibit critical targets such as DNA repair enzymes.
These derivatives have shown significant activity against cancer.
Conclusion: In cancer therapy, Quinazoline derivatives seems to be quite promising and act through various
mechanisms that are well established. This review has shown that quinazoline derivatives can further be explored
for the betterment of chemotherapy. A lot of potentials are still hidden, which demands to be discovered
for upgrading quinazoline derivatives efficacy.
