Betulin and betulinic acid are natural products readily isolated from the bark of birch trees. Betulinic acid has been found to possess selective toxicity towards cancer cells while being relatively non-toxic towards healthy cells.  The ready availability and favorable therapeutic index makes betulinic acid an attractive candidate for drug development.  Previously, we had reported the synthesis of betulinic acid analogs using reactions such as aldol condensation, Passerini reaction, and reductive amination.  Recently, we also reported the preparation of triazole conjugates of betulinic acid employing click chemistry and identified two series of these conjugates for further development as potential anti-cancer agents.  This poster will detail our recent efforts on the detailed SAR of these analogs.

Synthesis and cytotoxicity of Baylis-Hillman reaction derived betulinic acid analogs

254th National Meeting (2017)

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