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Cancer is the leading cause of the death since last few decades leading to the death of millions of people worldwide. Cancer is a generic term for a large group of diseases characterized by the growth of abnormal cells beyond their usual boundaries that can then invade adjoining parts of the body and/or spread to other organs. Also as the medication available is leading to the resistance, thus the continuous supply of new and novel anticancer drugs is the demand of the current situation. Derivatizing the existing anticancer drugs is an important strategy for the development of new anticancer agents. Lapatinib is 4-anilinoquinazoline derivative a dual tyrosine kinase inhibitor, acts by disrupting the epidermal growth factor receptor and HER2/neu pathways. Many derivatives of the lapatinib were previously reported by modification on quinazoline ring such as furanopyrimidine thiophenopyrimidine were found to be promising anticancer agents. Many isoxazole and isoxazolines derivatives have been reported for their anticancer potential, but the fused ring of isoxazole and pyrimidine is not yet explored for anticancer potential.

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