Abstract
Synthesis, Characterization and Cytotoxic Activity of Betulinic Acid and Seco-Betulinic Acid Derivatives against Human Colorectal Carcinoma
Mohd Tajudin Mohd Ali1, Habsah Zahari1, Aisyah Aliasak1, Siong Meng Lim2,3, Kalavathy Ramasamy2,3 and Allan Patrick G. Macabeo4
DOI : http://dx.doi.org/10.13005/ojc/330128
Abstract:
Different derivatives based on the betulinic acid triterpenoidal scaffold were synthesized and characterized spectroscopically. The derivatives including synthetic intermediates were evaluated for their cytotoxic activity against the human colorectal carcinoma cell line (HCT116) using a colorimetric sulforhodamine assay (SRB). Among the synthesized compounds, compound 6 featuring a 20-keto seco-betulinic acid conjugated with a lactone benzyl ester through an amide linkage at C-28, exhibited the lowest IC50 value.
Keywords:betulinic acid; seco-betulinic acid; lactone derivatives; ester derivatives; cytotoxicity; cancer
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