53773-09-4Relevant academic research and scientific papers
Heterocyclic IDH mutant inhibitor, preparation method and application thereof
-
, (2020/09/23)
The invention discloses a heterocyclic IDH mutant inhibitor, a preparation method and application thereof, belongs to the field of medicines, and particularly relates to a s-triazine compound with structural characteristics of a general formula (I) or a pharmaceutically acceptable salt thereof, a pharmaceutical composition, a preparation method of the s-triazine compound, and application of the s-triazine compound or the pharmaceutically acceptable salt and the pharmaceutical composition as isocitrate dehydrogenase 2 (IDH2) mutant inhibitors. The compound disclosed by the invention has an obvious inhibiting effect on the activity of an IDH2 mutant (mIDH2), can effectively inhibit the process of catalyzing alpha-ketoglutaric acid to generate 2-hydroxyglutaric acid by the mIDH2, and can be used for preventing and/or treating various related diseases including cancers caused by IDH2 mutation.
Identification and optimization of inhibitors of trypanosomal cysteine proteases: Cruzain, rhodesain, and TbCatB
Mott, Bryan T.,Ferreira, Rafaela S.,Simeonov, Anton,Jadhav, Ajit,Ang, Kenny Kean-Hooi,Leister, William,Shen, Min,Silveira, Julia T.,Doyle, Patricia S.,Arkin, Michelle R.,McKerrow, James H.,Inglese, James,Austin, Christopher P.,Thomas, Craig J.,Shoichet, Brian K.,Maloney, David J.
supporting information; experimental part, p. 52 - 60 (2010/04/29)
Trypanosoma cruzi and Trypanosoma brucei are parasites that cause Chagas' disease and African sleeping sickness, respectively. Both parasites rely on essential cysteine proteases for survival: cruzain for T. cruzi and TbCatB/rhodesain for T. brucei. A rec
