2898-56-8Relevant academic research and scientific papers
A kind of LSD1 inhibitors and use thereof
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, (2019/07/04)
The invention relates to novel LSD1 inhibitors and application of the LSD1 inhibitors in drugs, in particular to application of the LSD1 inhibitors in preparing LSD1-resistant inhibitor drugs, drugs for treating tumor, virus infectious diseases, hematolog
Design, synthesis, and biological evaluation of bromophenol derivatives as protein tyrosine phosphatase 1B inhibitors
Jiang, Bo,Shi, Dayong,Cui, Yongchao,Guo, Shuju
, p. 444 - 453 (2012/08/27)
3-Bromo-4,5-bis(2,3-dibromo-4,5-dihydroxybenzyl)-1,2-benzenediol (BDB) is a bromophenol purified from the marine red alga Rhodomela confervoides and exhibits potent protein tyrosine phosphatase 1B (PTP1B) inhibition (IC 50 = 1.7 μmol/L). In an effort to improve the PTP1B inhibitory activity, a series of derivatives were designed, synthesized, and evaluated in vitro. The preliminary structure-activity relationship indicated that the tricyclic scaffold and multi-bromine atoms (four to five) attached to the aryl rings are important for PTP1B inhibition. Among these, compound 26 exhibited remarkable inhibitory activity against PTP1B with an IC50 of 0.89 μmol/L, which was approximately two-fold more potent than the initial lead compound BDB.
COMPOUNDS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES
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Page/Page column 55, (2012/09/21)
Compounds and their pharmaceutically acceptable salts for treatment of synucleinopathies, such as Parkinson's disease and tauopathies.
Bromophenols as inhibitors of protein tyrosine phosphatase 1B with antidiabetic properties
Shi, Dayong,Li, Jing,Jiang, Bo,Guo, Shuju,Su, Hua,Wang, Tao
, p. 2827 - 2832 (2012/06/01)
A series of bromophenol derivatives were synthesized and evaluated as protein tyrosine phosphatase 1B (PTP1B) inhibitors in vitro and in vivo based on bromophenol 4e (IC50 = 2.42 μmol/L), which was isolated from red algae Rhodomela confervoides
