Background: 2-Furanones have attracted great attention due to their biological activities.
They also have the ability to be converted to several biologically active heterocyclic and nonheterocyclic
compounds, especially as anti-cancer agents.
Objectives: This research aims to share in the development process of novel cytotoxic agents by synthesizing
certain 2-furanone derivatives and using them as starting materials for the preparation of
novel heterocyclic and non-heterocyclic compounds, then testing the synthesized derivatives for their
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 the higher activity against several cell lines; 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 has 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 modification and investigations.