7073-36-1Relevant articles and documents
Synthesis and Antiproliferative Activities of Novel Substituted 5-Anilino-α-Glucofuranose Derivatives
Hou, Qiaoli,Li, Baolin,Li, Xiabing,Sun, Baoli,Wang, Lili,Wang, Wei,Zhang, Yaling
, (2020/05/05)
In order to find novel antitumor candidate agents with high efficiency and low toxicity, 14 novel substituted 5-anilino-α-glucofuranose derivatives have been designed, synthesized and evaluated for antiproliferative activities in vitro. Their structures were characterized by NMR (1H and 13C) and HR-MS, and configuration (R/S) at C(5) was identified by two-dimensional 1H,1H-NOESY-NMR spectrum. Their antiproliferative activities against human tumor cells were investigated by MTT assay. The results demonstrated that most of the synthesized compounds had antiproliferative effects comparable to the reference drugs gefitinib and lapatinib. In particular, (5R)-5-O-(3-chloro-4-{[5-(4-fluorophenyl)thiophen-2-yl]methyl}anilino)-5-deoxy-1,2-O-(1-methylethylidene)-α-glucofuranose (9da) showed the most potent antiproliferative effects against SW480, A431 and A549 cells, with IC50 values of 8.57, 5.15 and 15.24 μm, respectively. This work suggested 5-anilino-α-glucofuranose as an antitumor core structure that may open a new way to develop more potent anti-cancer agents.
Design and synthesis of arylamidine derivatives as serotonin/norepinephrine dual reuptake inhibitors
Wen, Hui,Qin, Wen,Yang, Guangzhong,Guo, Yanshen
, (2019/02/03)
To improve the in vivo antidepressant activity of previously reported serotonin (5-HT) and norepinephrine (NE) dual reuptake inhibitors, three series of arylamidine derivatives were designed and synthesized. The in vitro 5-HT and NE reuptake inhibitory activities of these compounds were evaluated, and compound II-5 was identified as the most potent 5-HT (IC50 = 620 nM) and NE (IC50 = 10 nM) dual reuptake inhibitor. Compound II-5 exhibited potent antidepressant activity in the rat tail suspension test and showed an acceptable safety profile in a preliminary acute toxicity test in mice. Our results show that these arylamidine derivatives exhibit potent 5-HT/NE dual reuptake inhibition and should be explored further as antidepressant drug candidates.
Diarylamino glucosan derivative, and preparation method and anti-tumor purpose thereof
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Paragraph 0108; 0109; 0110; 0111; 0122; 0133, (2017/04/26)
The invention belongs to the field of medicinal chemistry, and particularly relates to a diarylamino glucosan derivative, and a preparation method and an anti-tumor purpose thereof, wherein the diarylamino glucosan derivative particularly relates to a compound shown as a formula I. The invention also relates to the preparation method of the diarylamino glucosan derivative, and the purpose of the diarylamino glucosan derivative in an aspect of preparing medicine for treating tumor diseases. The diarylamino glucosan derivative particularly has the obvious inhibition effects on human skin quamous cell carcinoma cells, human lung carcinoma cells and human colon cancer cells.