Synthesis and Anticancer Activities of 5,6,7-Trimethylbaicalein Derivatives

概要

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The aim of this study was to develop potential anticancer agents based on a naturally occurring baicalein, a flavonoid from Scatellariae radix. Cinnamic acid derivatives were converted to corresponding chlorides and then condensed with 3, 4, 5-trimethoxyphenol in the presence of BF_3-Et_2O to give chalcones. Intramolecular cyclization of these intermediates by the actions of DMSO/I_2 afforded the desired trimethylbaicalein derivatives. Cell viability after treatment with the tested compound for 2 d was determined by a colorimetric MTT assay. The results indicated that most of the derivatives showed improved inhibition of proliferation of Hep G2 cells. Compound 9 was the most potent, in which the cell viability was reduced to < 2% at the 25μм level. In the case of Hep 3B cells, 8a, 8b and 8f showed moderate inhibition of their proliferation and 25μм was required to reduce the viability to ca. 30%. On the other hand, prostate DU145 cells were more resistant. Most of the derivatives caused a 60% inhibition of DU145 cells only at a concentration of 100μм or above.
公益社団法人日本薬学会の論文
2004-10-01