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Title:
NOVEL CDK9 INHIBITOR BASED ON BENZOPYRAN STRUCTURE, PREPARATION METHOD THEREFOR AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2020/228513
Kind Code:
A1
Abstract:
The present invention relates to the field of biomedicine, and specifically comprises a series of derivatives of a novel CDK9 inhibitor having a benzopyran structure and use thereof. In view of the disadvantages of low anti-tumor activity and poor druggability of wogonin, the present invention modifies the mother nucleus thereof to synthesize a series of compounds, especially introduces N-containing cyclic substituents at the 3- or 4-position. These compounds are all novel, and have not been reported in the literature. At the same time, the inventors carried out a series of biological activity evaluation on the synthesized compounds. In particular, most of the compounds of the present invention have good selectivity for CDK9, and have better inhibitory activity against cancer cells.

Inventors:
BIAN JINLEI (CN)
LI ZHIYU (CN)
ZHAO TENGTENG (CN)
WANG JUBO (CN)
WU TIZHI (CN)
TIAN YUCHENG (CN)
Application Number:
PCT/CN2020/086917
Publication Date:
November 19, 2020
Filing Date:
April 26, 2020
Export Citation:
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Assignee:
UNIV CHINA PHARMA (CN)
International Classes:
C07D311/30; A61K31/496; A61K31/5377; A61K31/541; A61K31/551; A61P31/14; A61P31/16; A61P31/18; A61P31/20; A61P35/00; A61P35/02; C07D405/04; C07D405/12; C07D405/14; C07D407/12; C07D417/12
Foreign References:
CN1668613A2005-09-14
CN110028475A2019-07-19
CN101472888A2009-07-01
EP0366061A11990-05-02
Attorney, Agent or Firm:
NANJING SUGAO PATENT AND TRADEMARK FIRM ( ORDINARY PARTNERSHIP ) (CN)
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