Synthesis and cytotoxic evaluation of ester analogues of (-)-curine

Abstract

This study presents the synthesis and cytotoxic evaluation of ester analogues derived from (-)-curine, a natural compound isolated from the roots of Cissampelos pareira (Menispermaceae). The synthesis involved the preparation of mono- and di-acetylcurine, along with four other ester derivatives, through diverse chemical transformations. Structural characterization of the synthesized compounds was performed using spectroscopic techniques and high-resolution mass spectrometry. Cytotoxicity assessments were conducted across various cancer cell lines, including MCF-7, MDA-MB-231, and Huh-7, as well as non-cancerous HEK293T cells, utilizing the MTT assay. Notably, compounds 4 and 5 demonstrated significant cytotoxic activities superior to the parent compound 1 and even matched or exceeded the cytotoxic effects induced by cisplatin, a conventional chemotherapeutic agent, across all tested cancer cell lines. These findings highlight the potential of compounds 4 and 5 as promising candidates for further development as potent cytotoxic agents in cancer therapy.