Synthesis And In Vitro Anti-tumor Activity Of Aromatic Acid Ester Derivatives Of Betulin

Betulin and betulinic acid are the main lupane pentacyclic triterpenoids in birch bark, the betulinic acid has unique anti-tumor and anti-HIV activity.Based on reported data, three-dimensional quantitative structure-activity relationship models, CoMFA and CoMSIA models on betulin derivatives structures and the antitumor activities were established in the present study.According to the molecular design principles, betulin was used as starting materials, aromatic acid ester derivatives of betulin were designed, synthesized, and identified by IR, NMR and MS.In vitro anticancer activities of these new compounds were tested against pancreatic cancer cell line MPC2, colon cancer cell line HT29, prostate cancer cell line DU145, lung carcinoma cell line NCI-H520, cervical carcinoma cell line HeLa, ovarian cancer cell lines2774. with betulinic acid as the positive control. The results showed that28-O-benzoyl betulin and28-O-benzene sulfonyl betulin has low cytotoxic activity, whereas28-O-(2’-carboxyl) benzoyl betulin displayed stronger antitumor activity which is valuable for further study.