Synthesis of Ring A-Modified Baicalein Derivatives

被引：13
|
作者：
Wang, Jun-Fei [2 ]
Ding, Ning [1 ]
Zhang, Wei [1 ]
Wang, Peng [2 ]
Li, Ying-Xia [1 ]
机构：
[1] Fudan Univ, Sch Pharm, Dept Med Chem, Shanghai 201203, Peoples R China
[2] Ocean Univ China, Sch Pharm, Key Lab Marine Drugs, Ministrat Educ China, Qingdao 266003, Peoples R China
来源：
HELVETICA CHIMICA ACTA | 2011年 / 94卷 / 12期
基金：
中国国家自然科学基金;
关键词：
Scutellaria baicalensis; Baicalein; O-Alkylation; O-Acylation; SCUTELLARIA-BAICALENSIS; LIPOXYGENASE INHIBITORS; CELL-LINES; IN-VITRO; FLAVONOIDS; APOPTOSIS; WOGONIN; RADIX; MECHANISMS; INDUCTION;
D O I：
10.1002/hlca.201100162
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
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, 226 (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.
引用
收藏
页码：2221 / 2230
页数：10
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