140406-65-1Relevant articles and documents
Preparation and application of sulfanilamide and benzothiazole compounds containing tetrahydroisoquinoline
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Paragraph 0026-0027, (2020/04/17)
The invention discloses a sulfanilamide compound, containing tetrahydroisoquinoline, shown as figure 1, and a benzothiazole compound, containing tetrahydroisoquinoline, shown as figure 2, and application of the sulfanilamide compound and the benzothiazole compound as novel protein arginine methyltransferase 5 inhibitors.
PRMT5 INHIBITORS AND USES THEREOF
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Paragraph 0212-0213, (2019/04/05)
Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666
Duncan, Kenneth W.,Rioux, Nathalie,Boriack-Sjodin, P. Ann,Munchhof, Michael J.,Reiter, Lawrence A.,Majer, Christina R.,Jin, Lei,Johnston, L. Danielle,Chan-Penebre, Elayne,Kuplast, Kristy G.,Porter Scott, Margaret,Pollock, Roy M.,Waters, Nigel J.,Smith, Jesse J.,Moyer, Mikel P.,Copeland, Robert A.,Chesworth, Richard
supporting information, p. 162 - 166 (2016/03/01)
The recent publication of a potent and selective inhibitor of protein methyltransferase 5 (PRMT5) provides the scientific community with in vivo-active tool compound EPZ015666 (GSK3235025) to probe the underlying pharmacology of this key enzyme. Herein, we report the design and optimization strategies employed on an initial hit compound with poor in vitro clearance to yield in vivo tool compound EPZ015666 and an additional potent in vitro tool molecule EPZ015866 (GSK3203591).