Journal of Guangxi Normal University(Natural Science Edition) ›› 2013, Vol. 31 ›› Issue (1): 62-66.

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Synthesis and Anti-tumor Activity Evaluation of Estradiol Ester Derivatives

LIU Guan-yan, CHENG Ke-guang, DENG Sheng-ping, LIU Yan-cheng, CHUXiang-wu, CHEN Jian-hui, MA Lu   

  1. Key Laboratory for the Chemistry and Molecular Engineering ofMedicinal Resources,Ministry of Education of China, College of Chemistry and Chemical Engineering,Guangxi Normal University,Guilin Guangxi 541004,China
  • Received:2012-09-13 Online:2013-03-20 Published:2018-11-26

Abstract: Estradiol ester derivatives were synthesized startingfrom estradiol and cinnamoyl chloride or ethyl succinyl chloride by esterfication to obtain fourtarget compounds.Their abilities to inhibit the tumor cell lines in vitro werestudied.The results of anti-tumor activity evaluation indicated that compounds1 and 3 which contained cinnamic acid ester group and 3-phenolic hydroxyl groupor 17-alcoholic hydroxyl group in estradiol free were much stronger in the inhibitory activity against tested tumor cell lines than that of 5-FU.The cinnamatecompound 1 which contained 3-phenolic hydroxyl group in estradiol free exhibited inhibition rate up to 73.91% and 67.93% respectively against breast cancer cell lines MCF-7 and MDA-MB-231.

Key words: estradiol, cinnamate, succinic acid monoethyl ester, anti-tumor

CLC Number: 

  • O629.23
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