Title:
MANNICH BASE DERIVATIVE OF ACETYLCHRYSIN AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2017/215538
Kind Code:
A1
Abstract:
Provided are a Mannich base derivative of acetylchrysin having a structrue of general formula I and a use thereof, wherein R1 and R2 are each independently selected from an acetyl and organic secondary amine methylene, and only one of R1 and R2 is an acetyl. Such a compound is a hypoxia-inducible transcription factor (HIF-1α) inhibitor regulated by a reactive oxygen species (ROS), which uses the different mechanisms of oxidation and reduction within normal cells and tumour cells, by capturing intracellular oxygen free radicals, specifically increasing the level of hydrogen peroxide in tumour cells, activating an intracellular apoptosis pathway, and knowing the death receptor pathway, and thus selectively inducing tumour cell apoptosis and inhibiting proliferation and metastasis, and protecting normal cells. Such a compound has a good druggability by oral administration, unique pharmacokinetic properties, a high efficiency and low toxicity, a clear mechanism of action, a good selectivity for solid tumours, rich sources of synthetic raw materials, a simple process, a high purity and a low cost.
Inventors:
ZHANG FAN (CN)
ZHANG SHIXUAN (CN)
JU XIULAN (CN)
ZHANG SHIXUAN (CN)
JU XIULAN (CN)
Application Number:
PCT/CN2017/087864
Publication Date:
December 21, 2017
Filing Date:
June 12, 2017
Export Citation:
Assignee:
ZHANG FAN (CN)
International Classes:
C07D405/06; A61K31/352; A61K31/4025; A61K31/453; A61K31/496; A61K31/5377; A61K31/541; A61P35/00; C07D311/30
Foreign References:
| CN106117189A | 2016-11-16 | |||
| CN1427003A | 2003-07-02 | |||
| CN101591322A | 2009-12-02 | |||
| CN101148444A | 2008-03-26 | |||
| CN1673222A | 2005-09-28 |
Other References:
LI, HAILIANG: "Structure Design Synthesis and Characterization of 6-Acetyl-Chrysin Mannich Base Derivatives", CHINA MASTER'S THESES FULL-TEXT DATABASE, 15 March 2017 (2017-03-15)
HU , KUN ET AL.: "Synthesis and Anticancer Activity of Chrysin Mannich Base Derivatives", JOURNAL OF SHENYANG PHARMACEUTICAL, vol. 27, no. 6, 20 June 2010 (2010-06-20), pages 448 - 452, ISSN: 1006-2858
MOHAMMED, H.A. ET AL.: "Facile Synthesis of Chrysin-Derivatives with Promising Activities as Aromatase Inhibitors", NATURAL PRODUCT COMMUNICATIONS, vol. 6, no. 1, 31 December 2011 (2011-12-31), pages 31 - 34, ISSN: 1394-578X
HU , KUN ET AL.: "Synthesis and Anticancer Activity of Chrysin Mannich Base Derivatives", JOURNAL OF SHENYANG PHARMACEUTICAL, vol. 27, no. 6, 20 June 2010 (2010-06-20), pages 448 - 452, ISSN: 1006-2858
MOHAMMED, H.A. ET AL.: "Facile Synthesis of Chrysin-Derivatives with Promising Activities as Aromatase Inhibitors", NATURAL PRODUCT COMMUNICATIONS, vol. 6, no. 1, 31 December 2011 (2011-12-31), pages 31 - 34, ISSN: 1394-578X
Attorney, Agent or Firm:
DALIAN GEZHI INTELLECTUAL PROPERTY AGENT LTD. (CN)
Download PDF:
Previous Patent: METHOD AND APPARATUS FOR UPDATING LINK STATE OF COMMUNICATION PORT
Next Patent: OPTICAL FIBER CONNECTOR
Next Patent: OPTICAL FIBER CONNECTOR