404597-94-0Relevant articles and documents
Discovery of flavonoids from scutellaria baicalensis with inhibitory activity against PCSK 9 expression: Isolation, synthesis and their biological evaluation
Nhoek, Piseth,Chae, Hee-Sung,Masagalli, Jagadeesh Nagarajappa,Mailar, Karabasappa,Pel, Pisey,Kim, Young-Mi,Choi, Won Jun,Chin, Young-Won
, (2018)
Nine flavonoids were isolated and identified from a chloroform-soluble fraction of the roots of Scutellaria baicalensis through a bioactivity-guided fractionation using a proprotein convertase subtilisin/kexin type 9 (PCSK9) monitoring assay in HepG2 cell
Polymethoxy flavone derivative with anti-hepatitis A virus activity as well as preparation method and application of polymethoxy flavone derivative
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Paragraph 0026; 0029, (2021/06/26)
The invention belongs to the field of medicinal chemistry, and relates to a polymethoxy flavone derivative with anti-hepatitis A virus activity as well as a preparation method and application of the polymethoxy flavone derivative. The polymethoxylated fla
The winding road of the uvaretin class of natural products: From total synthesis to bioactive agent discovery
Dallman, Johnathan,Lansakara, Ashabha,Nguyen, Thi,Weeramange, Chamitha,Hulangamuwa, Wasundara,Rafferty, Ryan J.
, p. 1420 - 1431 (2019/08/21)
Herein, we disclose the development of a synthetic route to gain access to the uvaretin class of chalcone natural products. In this, the construction of a small library was achieved, and the collection was evaluated for cytotoxicity and other biological properties. Uvaretin (1) was accessed via a seven-step route in an overall yield of 15.1%. Within this route, the unsaturated enone variant of uvaretin (2), also a natural product, was accessed in a 16.7% yield over six steps. This route provides a nearly three-fold increase in yields of 1 and 2 in comparison to the previous synthetic route accessing them in 5.8% and 3.0% overall yields, respectively. Evaluation of 1 and 2 revealed IC50 values between 2.0 and 5.1 μM in the cancerous cell lines HeLa, U937, A549, and MIA PaCa-2. Screening of the whole chalcone library set led to the discovery of over 30 compounds, within six cancerous cell lines, possessing single digit μM IC50 activity as sole agents. Furthermore, multiple library members were found to possess promising potentiating properties with known chemotherapeutic agents.