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Clusianone ( 1 ) was isolated from Garcinia parvifolia and structurally modified using semisynthetic methods to obtain compounds 2 – 4 . The structural derivatization included methylation ( 2 ), hydrogenation ( 3 ), and the addition of a methylamine group [( 4 ) to ( 1 )]. Cytotoxic effects of these compounds were assessed on MRC5 fibroblasts, A549 lung adenocarcinoma, HK1 squamous nasopharynx carcinoma, and NP69 normal nasopharyngeal epithelial cell lines. Clusianone ( 1 ) showed cytotoxic activity against A549 cells with an IC 50 value of 3.06 µM. Compound ( 4 ) showed cytotoxic activities against both A549 and HK1 cells with IC 50 values of 4.09 µM and 3.43 µM, respectively. The results of the cytotoxicity assay provide a correlation on the structure activity relationship of clusianone against HK1 and A549 cells, which can be further investigated as a potential antiproliferative compound.

Structural Derivatization of Clusianone and In Vitro Cytotoxicity Evaluation Targeting Respiratory Carcinoma Cells