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Medicinal Chemistry

Author(s): Rania Helmy Abd El-Hameed*, Hend Medhat El-Shanbaky and Mosaad Sayed Mohamed

DOI: 10.2174/1573406417666210604103135

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

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Abstract

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 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 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.

Keywords: 2-furanone, 2-pyrrolone, pyridazinone, synthesis, anti-cancer activity, MAPK14 inhibitor.

Graphical Abstract

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