99421-30-4Relevant academic research and scientific papers
Heterocyclic compounds as well as preparation method and application thereof
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Paragraph 0221; 0224; 0225, (2018/07/30)
The invention belongs to the field of medicines and particularly relates to heterocyclic compounds with the structural characteristics shown in formula (I) or pharmaceutically acceptable salts, a preparation method and an application of the heterocyclic compounds as a nucleotide oxidative damage repairase MTH1 inhibitor. Pharmacological experiment results indicate that the compounds have significant inhabitation effects on the activity of MTH1 and can be used for preventing and treating clinical diseases related to MTH1.
Synthesis and structure-activity relationship study of triazine-based inhibitors of the DNA binding of NF-κB
Fujii, Shinya,Kobayashi, Takanobu,Nakatsu, Aki,Miyazawa, Hiroshi,Kagechika, Hiroyuki
, p. 700 - 708 (2014/08/05)
Nuclear transcription factor nuclear factor-kappa B (NF-κB) has diverse pathophysiological functions, and NF-κ B inhibitors are considered to be candidates for multiple therapeutic applications. We previously reported a novel triazine-based NF-κB inhibitor, 2-anilino-4,6-dichloro-1,3,5- triazine (NI241), that directly inhibits DNA binding of NF-κB. Here, we report synthesis of a series of triazine derivatives and evaluation of their structure-activity relationships for NF-κB inhibition. We found that 2-amino-4,6-dichloro-1,3,5-triazine substructure is essential for the inhibitory activity of the lead compound NI241, and modification of NI241 by introduction of an m-methoxy substituent on the phenyl ring afforded the more potent derivative 28. The structure-activity relationships identified in this study suggested a possible mechanism of irreversible NF-κB inhibition by NI241, and should be helpful in the design of other NF-κB inhibitors.
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
