- 专利标题： Hybrid anticancer prodrug simultaneously producing cinnamaldehyde and quinone methide and method for preparing same
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申请号： US15109621申请日： 2015-01-05
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公开(公告)号： US09950071B2公开(公告)日： 2018-04-24
- 发明人: Dong Won Lee , Byoung Mog Kwon , Joung Youn Noh , Byeng Su Kwon , Dong Cho Han
- 申请人： INDUSTRIAL COOPERATION FOUNDATION CHONBUK NATIONAL UNIVERSITY , KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGY
- 申请人地址： KR Jeollabuk-Do
- 专利权人： Industrial Cooperation Foundation Chonbuk National University
- 当前专利权人： Industrial Cooperation Foundation Chonbuk National University
- 当前专利权人地址： KR Jeollabuk-Do
- 代理机构： Morrison & Foerster LLP
- 优先权： KR10-2014-0000653 20140103; KR10-2015-0000660 20150105
- 国际申请： PCT/KR2015/000067 WO 20150105
- 国际公布： WO2015/102448 WO 20150709
- 主分类号： C07D319/06
- IPC分类号： C07D319/06 ; A61K31/357 ; A61K47/48 ; A61K31/69 ; A61K9/00 ; A61K9/08 ; A23L33/10 ; A23L33/15 ; A23L33/155 ; A23L33/16 ; A61K47/26 ; A61K9/16 ; A61K9/20 ; C07F5/02 ; A61K47/55
摘要：
The present invention relates to a hybrid anticancer prodrug simultaneously producing cinnamaldehyde and quinone methide. The hybrid anticancer prodrug according to the present invention sequentially releases quinone methide and cinnamaldehyde by H2O2 and acidic pH, and thus alkylates antioxidant GSH through the release of quinone methide, thereby inhibiting an antioxidative system and increasing oxidation stress, and generates and accumulates reactive oxygen species (ROS) through the release of cinnamaldehyde, thereby promoting apoptosis, and thus the hybrid anticancer prodrug according to the present invention can be favorably used as an anticancer drug by creating a synergetic anticancer effect through double stimulus-response and sequential treatment action in a cancer cell-specific manner.