A series of rationally designed platanic acid‐based compounds derived from naturally occurring betulinic acid were synthesized through a sequence of Lemieux‐Johnson oxidation and Aldol condensation reaction. All the compounds were screened for cytotoxicity against a panel of human cancer and normal cell lines using MTT assay. From the biological data, it was observed that some of these semi‐synthetic congeners exhibited potent biological profiles compared to platanic acid. One of the compounds with the p‐tolyl substitution was found to be most active in this study, and its cytotoxicity against two of the cell lines, MDA‐MB 231 and A‐549 were in tune with the standard compound, 5‐fluorouracil.
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