Synthesis and anti-tumor activity of 30-hydroxy derivatives of 23-hydroxy betulinic acid

Aim:To improve the anti-tumor effects and to screen candidate for anti-tumor agent,30-hydroxy derivatives 6a-e and 7a were obtained from the modification of 23-hydroxy betulinic acid.Methods:After protection of the hydroxyl at C-3 and C-23 and carboxyl at C-28 of 23-hydroxy betulinic acid,the oxidation of compounds 5a-e was processed with m-chloroperoxybenzoic acid in chloroform by refluxing for 6 h.Meanwhile,the anti-tumor activity of the target compounds was tested by MTT.Results:The structures of the target compounds have been confirmed by the analytical and spectral analyses.The results showed that the anti-tumor activity of the target compounds was much potent than that of 23-hydroxy betulinic acid.Conclusion:The derivative of 23-hydroxy betulinic acid(6e) is a promising lead compound as the anti-tumor agent worth further investigation.