Title:
PHENYL ALLYLIDENE CYCLOHEXENONE DERIVATIVES AND PREPARATION METHOD AND USE
Document Type and Number:
WIPO Patent Application WO/2020/192348
Kind Code:
A1
Abstract:
Disclosed are phenyl allylidene cyclohexenone derivatives with the structure shown in general formula I. In combination with structural characteristics and structure-function relationship of piplartine, amino bonds are replaced with double bonds, and active groups are reserved, aromatic substituents are changed, novel phenyl allylidene cyclohexenone derivatives targeting thioredoxin reductase (TrxR) for tumor tissue overexpression are designed, the defects of multiple piplartine synthesis steps and requirement for expensive metal catalysts are overcome, and the anti-tumor activity of the compounds is improved. Research results indicate that the compounds have strong inhabitation effects on proliferation of tumor cells and can significantly increase the ROS level in the tumor cells and enhance the anti-tumor effect thereof.
Inventors:
LING YONG (CN)
YANG SHENGJU (CN)
ZHANG YAN'AN (CN)
LIU JI (CN)
LING CHANGCHUN (CN)
LI YANGYANG (CN)
LIU SIQUN (CN)
JIA QIXIN (CN)
MING GUXU (CN)
WU HONGMEI (CN)
YANG SHENGJU (CN)
ZHANG YAN'AN (CN)
LIU JI (CN)
LING CHANGCHUN (CN)
LI YANGYANG (CN)
LIU SIQUN (CN)
JIA QIXIN (CN)
MING GUXU (CN)
WU HONGMEI (CN)
Application Number:
PCT/CN2020/076878
Publication Date:
October 01, 2020
Filing Date:
February 27, 2020
Export Citation:
Assignee:
UNIV NANTONG (CN)
International Classes:
C07C49/683; A61P35/00; C07C45/74; C07C49/697; C07C49/747; C07C49/753; C07C69/157; C07C205/45; C07C225/22; C07C255/40
Domestic Patent References:
| WO2016014625A1 | 2016-01-28 |
Foreign References:
| CN110002987A | 2019-07-12 | |||
| CN102625805A | 2012-08-01 | |||
| CN106673988A | 2017-05-17 |
Other References:
CHANG, HSUN-SHUO ET AL.: "Antiproliferation of Cryptocarya concinna-derived cryptocaryone against oral cancer cells involving apoptosis, oxidative stress, and DNA damage.", BMC COMPLEMENTARY AND ALTERNATIVE MEDICINE., no. 16, 31 December 2016 (2016-12-31), XP055737391, ISSN: 1472-6882, DOI: 20200527142605A
Attorney, Agent or Firm:
NANJING IPLEADER INTELLECTUAL PROPERTY AGENCY FIRM (CN)
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