21.4

Conclusions

EGFR is a ligand-gated protein channel or biomolecule having a variety of cellular

functions in maintaining physiological processes. Alterations in the level of growth

factors or mutational modifications in the protein end up with many pathological

states including cancer. Although different EGFR inhibitors are available,

quinazoline-based anti-EGFR agents are of prime importance in current scenario.

Quinazoline is a medicinally active scaffold having a broad spectrum of pharmaco-

logical potential. Gefitinib and erlotinib are the first two quinazoline-based anti-

EGFR agents approved by the FDA in the years 2003 and 2004, respectively. After

the discovery of gefitinib and erlotinib as effective anti-EGFR agents, quinazoline-

based molecules or derivatives have attained a great interest in the field of anticancer

drug development. With steady efforts, four more quinazoline-based anti-EGFR

drugs were approved in the past few years. So till date, among 52 FDA-approved

molecules,

6

of

them

are

quinazoline-based

anti-EGFR

inhibitors.

Many

quinazoline-based novel and effective EGFR inhibitors designed and synthesized

in the past few years with a good inhibitory potential are represented in Table 21.1.

So, in this chapter, the different strategies to inhibit overexpressed or altered EGFR,

different compounds with good inhibitory potential developed in the past few years

and FDA-approved quinazoline-based anti-EGFR molecules are discussed in brief.

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21

EGFR-Targeted Quinazoline Clubbed Heterocycles as Anticancer Agents

397