Title:
D-3-PHOSPHOGLYCERATE DEHYDROGENASE ALLOSTERIC INHIBITOR AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2018/076537
Kind Code:
A1
Abstract:
Disclosed are a D-3-phosphoglycerate dehydrogenase allosteric inhibitor and the use thereof, wherein one class is the benzoyl hydrazine compound for the allosteric site MDL-1 of the enzyme, and the other class is the furan compound for the allosteric site MDL-2 of the enzyme. In vitro enzymatic activity tests, cell viability tests and mouse xenograft model experiments confirm that the two classes of allosteric inhibitors can specifically inhibit the activity of D-3-phosphoglycerate dehydrogenase and delay the growth of cancer cells by reducing the overexpression of the enzyme in cancer cells. Same are used alone or in combination, or in combination with other anti-cancer drugs and can treat, prevent or inhibit tumour diseases such as breast cancer, colon cancer, melanoma and non-small cell lung cancer.
Inventors:
LAI LUHUA (CN)
LIU YING (CN)
WANG QIAN (CN)
LIU PEI (CN)
LIU YING (CN)
WANG QIAN (CN)
LIU PEI (CN)
Application Number:
PCT/CN2016/113476
Publication Date:
May 03, 2018
Filing Date:
December 30, 2016
Export Citation:
Assignee:
UNIV BEIJING (CN)
International Classes:
A61K31/166; A61K31/341; A61K35/00; A61P35/00; C07D307/52
Domestic Patent References:
| WO2011069039A1 | 2011-06-09 |
Foreign References:
| CN106565643A | 2017-04-19 | |||
| US20100035932A1 | 2010-02-11 |
Attorney, Agent or Firm:
BEIJING WANXIANGXINYUE INTELLECTUAL PROPERTY OFFICE (CN)
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