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Epidermal Growth Factor Receptor (EGFR) Inhibitors for Tumor Anti-angiogenesis Activity
Published: 31 October 2012 by MDPI in The 16th International Electronic Conference on Synthetic Organic Chemistry session Bioorganic, Medicinal and Natural Products
Abstract: The EGFR family plays an essential role in normal organ development by mediating morphogenesis and differentiation through effects on cell proliferation, differentiation, apoptosis, invasion, and angiogenesis. Unlike normal cells that have tight regulatory mechanisms controlling EGFR pathways, tumor cells often have dysregulated EGFR signaling, allowing them to proliferate under adverse conditions, invade surrounding tissues, and increase angiogenesis. Epidermal growth factor receptor (EGFR) is a trans-membrane receptor tyrosine kinase that belongs to the Human epidermal receptor (HER) family of receptors. Receptor protein tyrosine kinases play a key role in signal transduction pathways that regulate cell division and differentiation. Among the growth factor receptor kinases that have been identified as being important in cancer is epidermal growth factor receptor (EGFR) kinase (also known as erb-B1 or HER-1) and the related human epidermal growth factor receptor HER-2 (also known as erbB-2). The quinazoline and other heterocyclic skeletons are of great importance to chemists as well as biologists as it is available in a large variety of naturally occurring compounds. In this article we are emphasizing on various hetericycles such as Quinazoline, pyrrolotriazines etc. as promising anticancer agents. These hetocycles showed the anticancer activity through the inhibition of EGFR enzyme. Attempt will be taken to provide details information on the said topic in the benefit of medicinal chemist.
Keywords: Anticancer agents, EGFR inhibitors, Heterocycles