Quinazoline Case Study

Quinazolines are the class of chemical compounds that are pharmacologically important as therapeutic agents. They are utilized as drugs and employed in cancer chemotherapy. They act by various mechanisms. Some of them act by inhibiting antifolat thymidylate syntheses, while some other derivatives inhibit tubulin polymerization. They were also found to inhibit the epidermal growth factor receptor (EGFR) tyrosine kinase over expression through the inhibition of autophosphorylation of EGFR. Further many quinazolines exhibit their antitumor properties by the inhibition of PARP-1 enzyme which is essential in DNA replication and repair. In olden days, quinazoline derivatives were exploited as antiviral, antiparkinsonism, antiinflammatory antimicrobial,
In this assay we examined the number of blood vessel formation and their subsequent inhibition by the derivatives. It was evident from the result that the selected derivatives H1 had reduced the number of vessels in comparison to control. It can be inferred that angiogenesis place a major role in the formation and development of tumors. Compounds exhibiting antiangiogenesis activity may be used as antitumor agents. Since the derivatives under study exhibited antiangiogenesis activity in CAM model, the compounds may be utilized in cancer
It was observed that the test compound showed minor cytotoxicity as compared to the positive control, and the IC50was found to be 110µgm192-93.
In last phase, it was planned to assess the anticancer activity of the selected quinazoline derivatives against MCF7 (Human breast cancer cell lines) and HCT116 (Human colon cancer cell lines) by MTT assay. In our experiment we observed that the test drug inhibits the proliferation of both types of cancer cell lines in a dose dependent manner. It was evident from the results that the quinazoline derivatives have the ability to inhibit the growth of cancerous cells as like doxorubicin did which was used as standard194-202.
Doxorubicin, a commonly used drug in the treatment of wide range of cancers, was used as a positive control in all our cytotoxic screening. The standard anticancer drug doxorubicin exhibited a stronger cytotoxic effect both on colon cancer cell lines and breast cancer cell lines. Its IC50 value was respectively found to be 4.7µg/ml and