185057-00-5Relevant articles and documents
Quinoline and Isoquinoline Based HDAC Inhibitors and Methods of Use Thereof
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Paragraph 0173; 0178, (2019/09/16)
The present invention relates to methods of modulating activity of histone deacetylases (HDACs). The present invention also relates to methods of treating HDAC-associated diseases including, but not limited to, cancers, inflammatory disorders, and neurode
Discovery of 2-substituted-N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)-1,2,3,4-tetrahydroisoquinoline-6-carboxamide as potent and selective protein arginine methyltransferases 5 inhibitors: Design, synthesis and biological evaluation
Shao, Jingwei,Zhu, Kongkai,Du, Daohai,Zhang, Yuanyuan,Tao, Hongrui,Chen, Zhifeng,Jiang, Hualiang,Chen, Kaixian,Luo, Cheng,Duan, Wenhu
, p. 317 - 333 (2019/01/04)
Protein arginine methyltransferases 5 (PRMT5) represents an attractive drug target in epigenetic field for the treatment of leukemia and lymphoma. Here, a series of N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)amide derivatives targeting PRMT5 were designed with structure-based approach and synthesized. Among them, compound 46 showed potent and selective PRMT5 inhibition activity with an IC50 of 8.5 nM, which was approximately equivalent with the phase I clinical trial PRMT5 inhibitor GSK-3326595 (IC50 = 5.5 nM). Compound 46 also displayed pronounced anti-proliferative activity in MV4-11 cells (GI50 = 18 nM) and antitumor activity in MV4-11 mouse xenografts model. This molecule can serve as an excellent tool compound for probing the biological function of PRMT5.
Pyrrolo pyrimidine ring compound, its use and pharmaceutical composition (by machine translation)
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Page/Page column 61; 62, (2017/07/31)
The invention relates to an as TLR7 agonist of the pyrrolo pyrimidine compounds, specifically on a compound of formula (I) compound or its pharmaceutically acceptable salt, preparation method thereof, containing the compounds of the pharmaceutical composition, and its use for the preparation of antiviral drug use. Formula (I) (by machine translation)