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Synthesis of Ring A-Modified Baicalein Derivatives

✍ Scribed by Jun-Fei Wang; Ning Ding; Wei Zhang; Peng Wang; Ying-Xia Li

Publisher
John Wiley and Sons
Year
2011
Tongue
German
Weight
237 KB
Volume
94
Category
Article
ISSN
0018-019X

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✦ Synopsis

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.

📜 SIMILAR VOLUMES

Glycyrrhetic acid derivatives with modif
Glycyrrhetic acid derivatives with modified ring A
✍ M. H. A. Elgamal; B. A. H. El-Tawil; M. B. E. Fayez 📂 Article 📅 1973 🏛 John Wiley and Sons 🌐 English ⚖ 164 KB

Ring A in glycyrrhetic acid (a therapeutically useful triterpenoid) was modified by contraction to an A-norhydroxy-acid derivative and by cleavage to a seco-A-2,3-dicarboxylic acid variant. Keyphrases 0 Glycyrrhetic acid derivatives-modification of ring A 0 Triterpenoid aglycones-modification of rin