GEM-DIFLUOROETHYL SUBSTITUTED STILBENE AND DIPHENYLETHANE DERIVATIVES, AND PREPARATION METHOD THEREFOR AND USE THEREOF

Title:

GEM-DIFLUOROETHYL SUBSTITUTED STILBENE AND DIPHENYLETHANE DERIVATIVES, AND PREPARATION METHOD THEREFOR AND USE THEREOF

Document Type and Number:

WIPO Patent Application WO/2019/020029

Kind Code:

A1

Abstract:

Disclosed are a gem-difluoroethyl substituted stilbene and diphenylethane derivatives, and a preparation method therefor and the use thereof. The present invention conducts a chemical structure modification with a gem-difluoroethyl at the 4' position of the B-aryl ring of diphenylethane/stilbene, and the 2' position thereof is modified into a substituent such as a nitro or amino. The gem-difluoroethyl substituted stilbene and diphenylethane derivatives have strong anti-tumour activity in vitro, with the anti-tumour activity of the trans-structure thereof better than that of the cis-structure thereof, and with the introduction of a fluorine atom not only changing the physical properties of the compounds themselves but also enhancing the anti-tumor activity in vitro, and have a good inhibitory effect on a variety of tumour cells. (I)

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Inventors:

WU FANHONG (CN)
MA ZHONGLIN (CN)
KAI ZHENPENG (CN)
HUANG LEILEI (CN)
LI DANDAN (CN)
HUANG JINWEN (CN)

Application Number:

PCT/CN2018/096870

Publication Date:

January 31, 2019

Filing Date:

July 24, 2018

Export Citation:

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Assignee:

SHANGHAI HUALI BIOMEDICAL CO LTD (CN)

International Classes:

C07C43/247; C07C211/26; C07F9/12; A61K31/09; A61K31/136; A61K31/661; A61P3/10; A61P19/02; A61P27/06; A61P31/00; A61P35/00

Foreign References:

CN107311846A	2017-11-03
CN108129325A	2018-06-08
CN108003032A	2018-05-08
CN104756984A	2015-07-08
CN1303294A	2001-07-11
CN101885738A	2010-11-17

Attorney, Agent or Firm:

SHANGHAI SSH INTELLECTUAL PROPERTY AGENCY CO., LTD. (CN)

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