Synthesis, Characterization, Docking Study and Biological Activates of New 3-Aminorhodanine Derivatives

Abstract

Abstract: Increase in fatalities among cancer patients is one of untreated facts and today cancer remains one of the main health issues. The most common cause of cancer death is lung cancer. Rhodanine has been recognized as a privileged scaffold in medicinal chemistry due to its well-known ability to demonstrate a broad range of biological activities, and most of its derivatives exhibited remarkable anticancer activity in the (μg/mL) concentration range, while causing negligible cytotoxicity to normal cells. New N- and 5- disubstituted aminorhodanine derivatives were synthesized by Schiff base and Knoevenagel condensation reactions over two consecutive steps. Human cancer cells and Hdfn (human dermal fibroblasts isolated from neonatal foreskin) cells line, were used to evaluate the synthesized compounds’ activity by MTT assay. The new compounds revealed higher anticancer activity against A549 lung cells cancer when compared with reference drug Erlotinib (anticancer drug) and determined no toxicity or safety on normal cell. Among the tested compounds, 2b2 compound show potent anticancer activity which have IC50 about (55.8 μg/mL).

Keywords

• EGFR mutantation
• Lung Cancer
• 3- aminorhodanine