The tyrosine klnase epidermal growth factor receptor (EGFR) has emerged in recent years as a key regulatory factor and validated target of targeted therapies for solid tumors. It plays a central role in oncology including activation of signaling pathways that regulate proliferation ; angiogenesis decreased apoptosis, and loss of differentiation. This work reviews the recent progress in inhibitors of epidermal growth factor receptor with alkylation properties. The alkylation groups and inhibiting mechanism are introduced, with an em- phasis on...