Title:
FUNCTIONAL CARBOHYDRATE MOLECULE BASED ON TDG MOLECULAR SCAFFOLD, AND PREPARATION METHOD THEREFOR
Document Type and Number:
WIPO Patent Application WO/2021/081881
Kind Code:
A1
Abstract:
The present invention provides a carbohydrate compound, the structure of which is as represented by formula X, wherein R1 and R2 are independently selected from a substituted amido group, a substituted triazolyl group, and a substituted amino group; R3 is selected from a sulfhydryl group, an azido group, an amino group, and a carboxyl group; A is formula aa or -CmH2mR3, wherein X is selected from an oxygen atom; n is selected from 0, 1, 2, 3, 4, 5, 6, and 7; m is selected from 2, 3, 4, 5, 6, 7, 8, 9, and 10. In the present invention, a synthesis strategy of "first side chain derivatization, then glycosylation coupling" is adopted, thereby achieving side chain derivatization modification of a TDG molecular scaffold and efficient synthesis of the compound . In the present invention , the use of the recognition and binding of a TDG glycoligand molecule to a target protein has a targeting function of identifying and binding to the target protein, and the TDG glycoligand molecule is used as a targeting molecule to construct a functional targeting molecule; the present invention has a wide application prospect in the fields such as tumor detection and tumor immunity.
Inventors:
LI WEI (CN)
WANG HUAIYU (CN)
WANG HUAIYU (CN)
Application Number:
PCT/CN2019/114660
Publication Date:
May 06, 2021
Filing Date:
October 31, 2019
Export Citation:
Assignee:
SHENZHEN INST ADV TECH (CN)
International Classes:
C07H19/056; G01N21/31; G01N21/78
Domestic Patent References:
| WO2016113335A1 | 2016-07-21 |
Foreign References:
| CN105158467A | 2015-12-16 | |||
| CN105241872A | 2016-01-13 | |||
| CN108602848A | 2018-09-28 | |||
| CN106536537A | 2017-03-22 |
Other References:
TAMARA DELAINE ET AL.: "Galectin-3-Binding Glycomimetics That Strongly Reduce Bleomycin-Induced Lung Fibrosis and Modulate Intracellular Glycan Recognition", CHEMBIOCHEM, vol. 17, no. 18, 12 August 2016 (2016-08-12), XP055527926, ISSN: 1439-4227, DOI: 10.1002/cbic.201600285
KRISTOFFER PETERSON ET AL.: "Systematic Tuning of Fluoro-galectin-3 Interactions Provides Thiodigalactoside Derivatives with Single-Digit nM Affinity and High Selectivity", JOURNAL OF MEDICINAL CHEMISTRY, vol. 61, no. 3, 28 December 2017 (2017-12-28), XP055527952, ISSN: 0022-2623, DOI: 10.1021/acs.jmedchem.7b01626
KRISTOFFER PETERSON ET AL.: "Systematic Tuning of Fluoro-galectin-3 Interactions Provides Thiodigalactoside Derivatives with Single-Digit nM Affinity and High Selectivity", JOURNAL OF MEDICINAL CHEMISTRY, vol. 61, no. 3, 28 December 2017 (2017-12-28), XP055527952, ISSN: 0022-2623, DOI: 10.1021/acs.jmedchem.7b01626
Attorney, Agent or Firm:
BEIJING CHENGHUI LAW FIRM (CN)
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