Utility of Certain 2-Furanone Derivatives for Synthesis of Different Heterocyclic Compounds and Testing their Anti-cancer Activity

Abstract

Background: 2-Furanones attracted great attention due to their biological activities. They also have the ability to convert to several biologically active heterocyclic and non-heterocyclic compounds, especially as anti-cancer agents. Objectives: This research aims to assist in the development process of novel cytotoxic agents through synthesizing certain 2-furanone derivatives, using them as starting materials for the preparation of novel heterocyclic and non-heterocyclic compounds, and then testing the synthesized derivatives for their anti-cancer activities. Methods: All the newly synthesized compounds were fully characterized by elemental analysis, IR, Mass, and 1H-NMR spectroscopy. 18 synthesized compounds were selected by National Cancer Institute (NCI) for testing against 60 cell lines, and the active compound was tested as MAPK14 and VEGFR2-inhibitor using Staurosporine as standard. Results: Compound 3a showed higher activity against several cell lines, including leukemia (SR), Non-Small Cell Lung Cancer (NCI-H460), colon cancer (HCT-116), ovarian cancer (OVCAR-4), renal cancer (786-0, ACHN and UO-31), and finally breast cancer (T-47D). It also had better inhibition activity against MAPK14 than the used reference. Conclusion: Compound 3a has promising anti-cancer activities compared to the used standards and may need further modifications and investigations.