4791-23-5Relevant articles and documents
Discovery of 5-Cyano-6-phenylpyrimidin Derivatives Containing an Acylurea Moiety as Orally Bioavailable Reversal Agents against P-Glycoprotein-Mediated Mutidrug Resistance
Wang, Bo,Ma, Li-Ying,Wang, Jing-Quan,Lei, Zi-Ning,Gupta, Pranav,Zhao, Yuan-Di,Li, Zhong-Hua,Liu, Ying,Zhang, Xin-Hui,Li, Ya-Nan,Zhao, Bing,Chen, Zhe-Sheng,Liu, Hong-Min
, p. 5988 - 6001 (2018)
P-glycoprotein (ABCB1)-mediated multidrug resistance (MDR) has become a major obstacle in successful cancer chemotherapy, which attracted much effort to develop clinically useful compounds to reverse MDR. Here, we designed and synthesized a novel series o
Design, Synthesis, and Antitumor Activity Evaluation of Trifluoromethyl-Substituted Pyrimidine Derivatives Containing Urea Moiety
Chao, Gao,Heyi, Yan,Honglin, Dai,Hongmin, Liu,Jiaxin, Zheng,Lihong, Shan,Limin, Liu,Luye, Zhang,Na, Li,Qiurong, Zhang,Tao, Wang,Xiujuan, Liu,Yang, Zhang,Zhengjie, Wang
, p. 1301 - 1311 (2021/12/23)
Abstract: In order to find efficient new antitumor drugs, a series of novel pyrimidine derivatives containing urea moiety were designed and synthesized, and the antitumor activity of four human tumor cells was evaluated by MTT analysis. The results showed that most of the target compounds exhibited moderate antitumor activity. In particular, the IC50 (concentration required to achieve 50% inhibition of the tumor cell proliferation) value of compound 2-((4-(4-ethylphenoxy)-6-(trifluoromethyl)pyrimidin-2-yl)thio)-N-((4-ethylphenyl)carba-moyl)acetamide for MGC-803 (human gastric carcinoma cell line) was 2.51 ± 0.17 μmol L–1, the anti-proliferative activity was significantly better than the positive control drug 5-fluorouracil. Molecular docking revealed that this compound can bind well to the active site of epidermal growth factor receptor (EGFR), and it may become a potential antitumor drug.
ANTIBACTERIAL THERAPEUTICS AND PROPHYLACTICS
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, (2017/02/24)
The present disclosure relates generally to novel molecules, compositions, and formulations for treatment of bacterial infections in general and more specifically to bacterial infections with antibiotic resistant pathogens.