Semisynthesis and Antitumor Activities of New Styryl-Lactone Derivatives

概要

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Nineteen new derivatives (2-20) of the naturally occurring compound, goniothalamin (1), were prepared by chemical modification and semi-synthetic methods. The antitumor activities of these derivatives and goniothalamin were evaluated in vitro against human tumor cell lines, and most of them showed an inhibitory effect against HL-60 cancer cells. The derivatives 10-nitro-goniothalamin (2) and 10-amino-goniothalamin (4) gave selective inhibition concentration (IC_<50>) of 1.10 and 1.14μg/ml, respectively, against human stomach cancer SGC-7901 cells, while that of etoposide (vp-16) as the positive control was 6.07μg/ml. Finally, the partition coefficients, logP (π values), of these derivative molecules, were evaluated by calculating the additive approximate organic fragment logP value.
公益社団法人日本薬学会の論文
2005-11-01