Abstract
AbstractBaicalein, an important active constituent of the traditional Chinese herbScutellaria baicalensis, exhibited antitumor activity and inhibitory activity against P‐gp 170. The syntheses of 25 baicalein derivatives,2–26(Table), are described here (Scheme 1). These compounds were systematically modified withO‐alkylation andO‐acylation at HOC(5), HOC(6), and HOC(7), singly or in combination, on the ringAof baicalein in order to evaluate the effects of such modifications on their inhibitory activities against multidrug‐resistant tumor cell lines and P‐gp 170. Highly selective and efficient alkylations at HOC(7) of peracetylated baicalein were the key to the distinction between HOC(6) and HOC(7) of baicalein.
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