1016-19-9Relevant articles and documents
Sulfonamide and urea-based anions chemosensors
Hu, Fang,Cao, Meijiao,Huang, Juanyun,Chen, Zhao,Wu, Di,Xu, Zhiqiang,Liu, Sheng Hua,Yin, Jun
, p. 108 - 115 (2015)
The detection of anions has attracted considerable interest because of their importance in various physiological processes. In this study, two sulfonamide and urea-based compounds (1a and 1b) were successfully developed and their spectroscopic and anion recognition properties were fully investigated. These results showed that: (1) compounds showed high selectivity towards cyanide and fluoride ions in CH3CN; (2) compounds only exhibited a large change in fluorescence in the presence of cyanide ions in CH3CN-H2O (95:5, v/v); and (3) compound 1b could act as a gel in dimethyl sulfoxide that transforms into a homogeneous solution upon exposure to cyanide ions. This research suggests that sulfonamide and urea can act as hydrogen-bond donors and provides an alternative approach to the design of novel anion chemosensors.
Novel 5-fluorouracil sensitizers for colorectal cancer therapy: Design and synthesis of S1P receptor 2 (S1PR2) antagonists
Luo, Dongdong,Guo, Zhikun,Zhao, Xuecui,Wu, Lijuan,Liu, Xiaochun,Zhang, Yingzhi,Zhang, Yuhang,Deng, Zirong,Qu, Xianjun,Cui, Shuxiang,Wan, Shengbiao
, (2021/10/25)
Sphingosine-1-phosphate receptor 2 (S1PR2) has been identified as a brand-new GPCR target for designing antagonists to reverse 5-FU resistance. We herein report the structural optimization and structure-activity relationship of JTE-013 derivatives as S1PR2 antagonists. Compound 9d was the most potent S1PR2 antagonist (KD = 34.8 nM) among developed compounds. Here, compound 9d could significantly inhibit the expression of dihydropyrimidine dehydrogenase (DPD) to reverse 5-FU-resistance in HCT116DPD and SW620/5-FU cells. Further mechanism studies demonstrated that compound 9d not only inhibited S1PR2 but also affected the transcription of S1PR2. In addition, compound 9d also showed acceptable selectivity to normal cells (NCM460). Importantly, compound 9d with suitable pharmacokinetic properties could significantly reverse 5-FU-resistance in the HCT116DPD and SW620/5-FU xenograft models without obvious toxicity, in which the inhibition rates of 5-FU were increased from 23.97% to 65.29% and 27.23% to 60.81%, respectively. Further immunohistochemistry and western blotting analysis also demonstrated that compound 9d significantly decreases the expression of DPD in tumor and liver tissues. These results indicated that compound 9d is a promising lead compound to reverse 5-FU-resistance for colorectal cancer therapy.
With anti-tumor effect of a quinazoline-urea derivative and its application (by machine translation)
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Paragraph 0139-0142; 0158, (2016/11/02)
The present invention relates to a of the general formula (II) anti-tumor function of said quinazoline-urea derivative and its application. The definition of the substituent in the general formula (II) in the specification. This invention, in order to SUO draw non-Buddhist nun and Geftinat compounds as the precursor, retention of SUO draw non-Buddhist nun the pharmocology-carbamido; at the same time, such as in reserved [...] EGFR-TKIs Geftinat, synthesis, and obtain a series of quinazoline-urea derivatives, by the in vitro activity tests, some compounds exhibit excellent anti-tumor activity, such derivatives have high research and utility value. (II). (by machine translation)