1058721-62-2Relevant academic research and scientific papers
Structure-based design and synthesis of small molecular inhibitors disturbing the interaction of MLL1-WDR5
Li, Dong-Dong,Chen, Wei-Lin,Xu, Xiao-Li,Jiang, Fen,Wang, Lei,Xie, Yi-Yue,Zhang, Xiao-Jin,Guo, Xiao-Ke,You, Qi-Dong,Sun, Hao-Peng
, p. 1 - 8 (2016)
MLL1 complex catalyzes the methylation of H3K4, and plays important roles in the development of acute leukemia harboring MLL fusion proteins. Targeting MLL1-WDR5 protein-protein interaction (PPI) to inhibit the activity of histone methyltransferase of MLL1 complex is a novel strategy for treating of acute leukemia. WDR5-47 (IC50 = 0.3 μM) was defined as a potent small molecule to disturb the interaction of MLL1-WDR5. Here, we described structure-based design and synthesis of small molecular inhibitors to block MLL1-WDR5 PPI. Especially, compound 23 (IC50 = 104 nM) was the most potent small molecular, and about 3-times more potent than WDR5-47. We also discussed the SAR of these series of compounds with docking study, which may stimulate more potent compounds.
5,6,7,8-TETRAHYDRO[1,2,4]TRIAZOLO[4,3-a]PYRAZINE DERIVATIVES AS P2X7 MODULATORS
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Page/Page column 99, (2010/11/17)
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof wherein A is hydrogen, C1-4alkyl, C3-6cycloalkyl, C1-3alkoxy, C1-3alkoxy C1-4alkyl, C1-2fluoroalkyl, halogen, NR6 R7, optionally substituted heteroaryl (Het), or optionally substituted phenyl, and R1, R2, R3, R4, R5, R6 and R7 are as defined in the description. The compounds or salts are thought to modulate P2X7 receptor function and to be capable of antagonizing the effects of ATP at the P2X7 receptor. The invention also provides the use of the compound or salt in the treatment or prophylaxis of, for example, inflammatory pain, neuropathic pain, visceral pain, rheumatoid arthritis, osteoarthritis or neurodegenerative disorders.
Potent 6-desfluoro-8-methylquinolones as new lead compounds in antibacterial chemotherapy
Cecchetti, Violetta,Fravolini, Arnaldo,Palumbo, Manlio,Sissi, Claudia,Tabarrini, Oriana,Terni, Patrizia,Xin, Tao
, p. 4952 - 4957 (2007/10/03)
In a furtherance of our SAR study on the C-6 position of quinolone antibacterials, a series of 6-desfluoro-8-methylquinolones were synthesized and evaluated for their in vitro antimicrobial activity. As a result of this study, compounds with strong activi
