Abstract
Nitrogen heterocyclic scaffold is one of very important derivatives in organic compounds, which possesses a wide range of biological activities and pharmacological activities and also has wide applications in many drugs, clinic trials and scientific researches. So, exploring fast and efficient synthetic methods of nitrogen heterocycles have been one of hot topics in organic chemistry. In this article, two series of 2-azetidinone analogues with potential antitumor activities were designed and synthesized via post-Ugi cascade reaction. The structures of the target molecules were characterized by 1H NMR, 13C NMR and HRMS spectra. The cancer cell lines LN229, MDA-MB-453, SW620, and DU145 were selected to evaluate the antitumor activity in vitro via MTT method. The results showed most compounds exhibited inhibitory activities against the cancer cells. Particularly, compounds 7e and 13e exhibited respectful antitumor activities in LN229 and DU145 cancer cell lines respectively with 53% inhibition, which are potential for further drug discovery.
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