Selective alkylation of β-anhydroicaritine and their biological evaluation on anticancer
期刊名：Natural Product Research
文献编号：
文献地址： https://www.tandfonline.com/doi/abs/10.1080/14786419.2020.1844686?journalCode=gnpl20
发表日期：10 Nov 2020
文献编号：
文献地址： https://www.tandfonline.com/doi/abs/10.1080/14786419.2020.1844686?journalCode=gnpl20
发表日期：10 Nov 2020
AbstractA convenient and selective alkylation of icaritin has been developed. The methodology involved initial formation of β-anhydroicaritine (3) under acidic conditions followed by selective methylation at the C-3 position and then alkylation at C-5 position. Several alkylated β-anhydroicaritine derivatives were synthesised using this methodology. These newly synthesised derivatives, especially the compounds 5b, 5c and 5j, significantly suppressed cell proliferation when tested against cancer cell lines in vitro. Compound 5j (R = Bn) exhibited a competitive inhibition against MCF7 in vivo compared to tamoxifen.
… TLC plates (GF 254) were bought from Branch Qingdao Haiyang Chemical Plant.
Icariin (98%) was bought from Biopurify Phytochemicals Ltd (Chengdu, China).
All the solvents are bought from Sinopharm. 4. Conclusion. In …
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