Review on the Significance of Quinazoline Derivatives as Broad Spectrum Anti-Cancer Agents.

Abstract

Cancer is one of the major causes of human mortality worldwide. A number of approved 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 explained 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. An interesting output of extensive research is that the quinazoline scaffold and its various derivatives can be explored further as a significant class of cancer chemotherapeutic agents that has already shown promising activities against different tumors. In general, quinazoline derivatives have already occupied a crucial place in modern medicinal chemistry. Quinazoline is one of the most studied moieties in medicinal chemistry due to the wide range of biological properties such as the anticancer, antibacterial, anti-inflammatory, antimalarial and antihypertensive activities. The anticancer activity of this scaffold has been well established.

New quinazolinone‐based derivatives as DHFR/EGFR‐TK inhibitors: Synthesis, molecular modeling simulations, and anticancer activity

“…The quinazoline-4-one scaffold-based anticancer compounds have been found to act through different molecular targets via inhibition of dihydrofolate reductase (DHFR), epidermal growth factor receptor tyrosine kinase (EGFR-TK), tubulins, and phosphatidylinositol 3-kinases. [11,12] DHFR is a vital enzyme in human physiology due to its significant role in cell growth and proliferation through the production of tetrahydrofolate (THF) required for the activity of folate-dependent enzymes, which are essential for DNA synthesis and methylation. [13][14][15][16] DHFR plays a crucial role in folate metabolism through the catalysis of NADPH-dependent reduction of dihydrofolate (DHF) to THF that is required for several one-carbon transfer reactions in purine and pyrimidine synthesis.…”