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DÉRIVÉ DE PODOPHYLLOTOXINE SUBSTITUÉ PAR SOUFRE-4, SON PROCÉDÉ DE PRÉPARATION ET SON UTILISATION
专利权人:
Tang; Yajie
发明人:
申请号:
EP18857722.5
公开号:
EP3686203A1
申请日:
2018.06.04
申请国别(地区):
EP
年份:
2020
代理人:
摘要:
Disclosed are a 4-sulfur substituted podophyllotoxin derivative and a synthetic method therefor and the use thereof. In the present invention, introducing heteroaromatic compounds with rigidity, such as 4-trifluoromethylpyridin-2-thiol, 4-trifluoromethyl-2-mercaptopyrimidine, and para-fluorothiophenol, respectively as substituent groups to position 4 of C ring of a podophyllotoxin or 4'-demethylepipodophyllotoxin, obtaining a podophyllotoxin derivative as shown in formula (V) with a significantly improved antitumour activity and reduced toxic side effects. Experiments of in vitro tumour cell activity inhibition indicate that the antitumour activity of the compound as shown in formula (V) of the present invention is significantly improved compared to that of the podophyllotoxin or 4'-demethylepipodophyllotoxin.
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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