Design and Synthesis of Some Novel Erlotinib Derivatives as Potential EGFR Kinase Inhibitors

Despite many significant improvements in cancer therapies over the past 50 years, metastatic solid cancers remain largely incurable. The survival for patients with these malignancies is often measured in months. Substantial efforts are being made in the development of targeted therapies for a specific type of cancer. These efforts have been spurred by few successes, such as imatinib for Chronic Myelogenous Leukaemia (CML); Trastuzumab for breast cancer with amplification of ERBB2 (also known as HER2); and erlotinib and gefitinib for lung cancer that regulates mutant epithelial growth factor receptor (EGFR). In the era of targeted drug discovery tyrosine kinases (TKIs) are the most studied pathways. The targeted drug discovery is preferable over conventional method and is used to reduce the maximum resistance and side effects. Especially with the EGFR mutation cause dramatic changes in patients. The mutations in the EGFR signalling pathway is one of the main reasons for one-third of non-small cell lung cancer.