Synthesis and Preliminary Antitumor Activities of 7(6)-Hydroxylflavone Derivatives

Five 7-hydroxylflavones and five 6-hydroxylflavones have been synthesized with resorcinol and paradioxybenzene as starting materials in three steps by an improved Baker-Venkatarama rearrangement reaction. Experimental results showed that the ten compounds have poor solubility in methanol and chloroform solvent and low biological activity. Therefore, some of these compounds are further derivatived and five new compounds were successfully synthesized. The nineteen compounds, including four new beta-propenediones 4b, 4c, 4d and 4e, were evaluated for antitumor activities against hela human cervical carcinoma cell lines by methyl thiazolyl tetrazolium (MTT) method. The preliminary biological activity tests showed that compound 13 exhibited potentially high activity against hela human cervical carcinoma cell lines with IC50 value of 19.4 mu mol/L.