Title:
O-PHENYL CHALCONE COMPOUND AND PREPARATION METHOD AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2015/109963
Kind Code:
A1
Abstract:
Disclosed are an o-phenyl chalcone compound and preparation method and use thereof The o-phenyl chalcone compound is capable of inhibiting the aggregation assembly of microtubules in tumour cells and influencing the mitosis of the cells, and has a high antitumour activity, and has the effect that the median inhibitory concentration of the proliferation inhibition on various tumour cells, such as a human ovary cancer cell A2780, a human colon cancer cell HCT8, a human breast cancer cell MCF7, a human lung cancer cell A549, a human colon cancer cell SW480, a human nasopharyngeal carcinoma cell CNE2, a human liver cancer cell HepG2 and the like, is mostly up to the level of nmol/l. In addition, the o-phenyl chalcone compound is capable of effectively resisting various multidrug resisting tumours resistant to clinical drugs, such as taxol, vinblastine, adriamycin and cisplatin; compared with the existing clinical representative drugs, such as adriamycin, taxol, colchicines and vincristine, the o-phenyl chalcone compound disclosed in the present invention not only has a remarkable advantage in the aspect of resisting drug-resistant tumours, but also has the important advantages of a novel structure, simple synthesis, cheap raw materials, good solubility and the like in the aspect of physicochemical properties.
Inventors:
BU XIANZHANG (CN)
ZHU CUIGE (CN)
YUE XIN (CN)
ZUO YINGLIN (CN)
CHEN YU (CN)
WEN GESI (CN)
ZHU CUIGE (CN)
YUE XIN (CN)
ZUO YINGLIN (CN)
CHEN YU (CN)
WEN GESI (CN)
Application Number:
PCT/CN2015/070651
Publication Date:
July 30, 2015
Filing Date:
January 14, 2015
Export Citation:
Assignee:
UNIV SUN YAT SEN (CN)
International Classes:
A61P35/00; C07F5/02; C07C45/45; C07C49/835; C07C49/84; C07C221/00; C07C225/22; C07C253/30; C07F9/12
Foreign References:
| CN102344351A | 2012-02-08 | |||
| PT73973A | 1981-12-01 |
Other References:
CUIGE ZHU ET AL.: "Discovery of potent cytotoxic ortho-aryl chalcones as new scaffold targeting tubulin and mitosis with affinity-based fluorescence", JOURNAL OF MEDICINAL CHEMISTRY, 25 July 2014 (2014-07-25), pages 6364 - 6382, XP055214375
Attorney, Agent or Firm:
YOGO PATENT & TRADE MARK AGENCY LIMITED COMPANY (CN)
广州粤高专利商标代理有限公司 (CN)
广州粤高专利商标代理有限公司 (CN)
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