Synthesis of Ring A‐Modified Baicalein Derivatives |
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| Authors: | Jun‐Fei Wang Ning Ding Wei Zhang Peng Wang Ying‐Xia Li |
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| Institution: | 1. Key Laboratory of Marine Drugs, The Ministration of Education of China, School of Pharmacy, Ocean University of China, 5 Yushan Road, Qingdao 266003, P.?R. China;2. Department of Medicinal Chemistry, School of Pharmacy, Fudan University, 826 Zhangheng Road, Shanghai 201203, P.?R. China, (phone: +86‐21‐51980127;3. fax: +86‐21‐51980127) |
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| Abstract: | Baicalein, an important active constituent of the traditional Chinese herb Scutellaria 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 with O‐alkylation and O‐acylation at HO? C(5), HO? C(6), and HO? C(7), singly or in combination, on the ring A of 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 HO? C(7) of peracetylated baicalein were the key to the distinction between HO? C(6) and HO? C(7) of baicalein. |
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| Keywords: | Scutellaria baicalensis Baicalein O‐Alkylation O‐Acylation |
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