Epidermal Growth Factor Receptor (EGFR) is a transmembrane glycoprotein that constitutes
one of the four members of ErbB family of tyrosine kinase receptors. Activation of EGFR leads to
autophosphorylation of receptor tyrosine kinase that initiates a cascade of downstream signaling
pathways involved in regulating cellular proliferation, differentiation, and survival. EGFR is abnormally
activated by various mechanisms like receptor overexpression, mutation, ligand-dependent receptor
dimerization, ligand-independent activation and is associated with the development of variety of
human cancers. EGFR inhibition is one of the key targets for cancer chemotherapy. Approval of tyrosine kinase inhibitors
such as erlotinib, gefitinib, and lapatinib for the treatment of non-small cell lung cancer led to tremendous development of
novel EGFR inhibitors in the last decade. Diverse class of chemical compounds from the synthetic origin has been
extensively studied. This review highlights the various classes of synthetically derived molecules which have been reported in
the last few years as potential EGFR and EGFR/ErbB-2 dual inhibitors. A brief synthetic methodology to access these
compounds has been highlighted along with the SAR. We strongly believe that this review will provide a platform to the
synthetic chemists and biologists to design and synthesize new and potent compounds that inhibit EGFR and ErbB-2.
Keywords: Antibodies, Apoptosis, Carcinoma, EGFR, Heterocyclic, Proliferation.
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