262375-99-5Relevant articles and documents
Phenylpiperazine type UBE2F small molecule inhibitor and synthesis method thereof
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, (2019/09/14)
The invention discloses a phenylpiperazine type UBE2F small molecule inhibitor and a synthesis method thereof, discloses a phenylpiperazine type compound represented by the general formula I or a pharmaceutically acceptable salt thereof, and further discloses a synthesis route of the general formula I and a synthesis method of each step. As a small molecule inhibitor target at UBE2F, that phenylpiperazine type compound of the present invention effectively suppresses the growth of tumor cell by preventing the G2/M process of cell cycle and inducing apoptosis of human tumor cells. Therefore, thecompound is a new class of specific anti-tumor drugs by targeting UBE2F.
Functionalized acridin-9-yl phenylamines protected neuronal HT22 cells from glutamate-induced cell death by reducing intracellular levels of free radical species
Nguyen, Thuy,Yang, Tianming,Go, Mei-Lin
, p. 1830 - 1838 (2015/03/14)
The in vitro neuronal cell death model based on the HT22 mouse hippocampal cell model is a convenient means of identifying compounds that protect against oxidative glutamate toxicity which plays a role in the development of certain neurodegenerative diseases. Functionalized acridin-9-yl-phenylamines were found to protect HT22 cells from glutamate challenge at submicromolar concentrations. The Aryl1-NHAryl2 scaffold that is embedded in these compounds was the minimal pharmacophore for activity. Mechanistically, protection against the endogenous oxidative stress generated by glutamate did not involve up-regulation of glutathione levels but attenuation of the late stage increases in mitochondrial ROS and intracellular calcium levels. The NH residue in the pharmacophore played a crucial role in this regard as seen from the loss of neuroprotection when it was structurally modified or replaced. That the same NH was essential for radical scavenging in cell-free and cell-based systems pointed to an antioxidant basis for the neuroprotective activities of these compounds.