Synthesis of 3鈥?methoxy-E-diethylstilbestrol and its analogs as tumor angiogenesis inhibitors

详细信息	查看全文 | 推荐本文 |

• 作者：Qian Liu^a ; Weiwei Jin^a ; Yan Zhu^b ; Jieyun Zhou^b ; Min Lu^a ; Qian Zhang^a ; ^{zhangqian511@shmu.edu.cn}
• 关键词：2-Methoxyestradiol ; 3&prime ; -Methoxy-E-diethylstilbestrol ; Metabolite ; Non-steroidal analog ; Angiogenesis inhibitor
• 刊名：Steroids
• 出版年：2012
• 期刊代码：142_0039128x
• 类别：bio
• 出版时间：April, 2012
• 卷：77
• 期：5
• 页码：419-423
• 文件大小：294 K

摘要

3鈥?Methoxy-E-diethylstilbestrol (2), with the structural and original similarities to 2-methoxyestradiol (2-ME2, 1), was synthesized and screened against HUVEC and a series of human cancer cell lines including RL95-2, SKOV-3, MCF-7 and T-47D in vitro. The configuration of the title compound was determined via the single crystal X-ray diffraction of its benzoyl-ester derivative (10). The fact that 3鈥?methoxy-E-diethylstilbestrol and its analogues (8 and 11) showed potential antiangiogenesis and anti-tumor activities at a close level, whereas its ester derivative (10) did not display any cytotoxic activities on all the screening cell lines indicated that the core scaffold of 3鈥?methoxy-3,4-diphenylhexane and the exposed hydroxyl-groups in the structures are essential pharmacophores for their anti-tumor activities.