125092-42-4Relevant articles and documents
Discovery of the theobromine derivative MQS-14 that induces death of MGC-803 cells mainly through ROS-mediated mechanisms
Ma, Ting,Ma, Qi-Sheng,Yu, Bin,Liu, Hong-Min
, p. 76 - 86 (2019)
Reactive oxygen species (ROS) play crucial roles in maintaining redox balance and regulating physiological processes, ROS levels in cancer cells are relatively higher than those in normal cells. Therefore, elevating cellular ROS levels may be a viable strategy for selective killing of cancer cells. In this work, we synthesized a series of new theobromine derivatives and evaluated their cytotoxicity against gastric cancer cells MGC-803, SGC-7901 and HGC-27. Particularly, MQS-14 potently inhibited cell growth of MGC-803, SGC-7901 and HGC-27 cells at low micromolar levels. Mechanistic studies showed that compound MQS-14 decreased cell viability of MGC-803 cells and inhibited cell division revealed by the CFDA and EdU staining assays. MQS-14 increased cellular ROS levels and activated the MAPK pathway accompanied by the decreased p-ERK and increased p-JNK expression. MQS-14 also induced DNA damage and apoptosis in MGC-803 cells. To conclude, MQS-14 induced cell death of MGC-803 cells partly through elevating cellular ROS levels.
Xanthine LSD1 inhibitor and preparation method and application thereof
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Paragraph 0017; 0043; 0044; 0048-0050, (2018/06/15)
The invention belongs to the field of medicinal chemistry, and discloses a xanthine structure containing LSD1 inhibitor, a synthesizing method and related application. The xanthine LSD1 inhibitor is characterized in that the structure formula is shown in the description, wherein R1 is benzyl; R2 is 1-3 alkyl and carboxylic acid derivates; R3 is heteroatom substituted hexatomic ring. The LSD1 enzymatic activity detection result shows that the xanthine compound of such series is good in effect on inhibiting LSD1 and can be used as a lead compound, and on that basis, a novel LSD inhibitor is further designed (refer to Specification).