129488-55-7Relevant academic research and scientific papers
Discovery of novel VEGFR-2 inhibitors embedding 6,7-dimethoxyquinazoline and diarylamide fragments
Wang, Ru,Liu, Hu,You, Yuan-Yuan,Wang, Xin-Yu,Lv, Bing-Bing,Cao, Li-Qin,Xue, Jia-Yu,Xu, Yun-Gen,Shi, Lei
supporting information, (2021/02/02)
VEGF/VEGFR-2 signaling plays a critical part in tumor angiogenesis. Inhibition of this pathway has been considered as a promising approach for cancer treatment. In this work, a series of 6,7-dimethoxy-4-anilinoquinazoline derivatives bearing diarylamide moiety were designed, synthesized and evaluated as potent inhibitors of VEGFR-2 kinase. Their in vitro antiproliferation activities against two human cancer cell lines Hep-G2 and MCF-7 have also been determined. Among them, compound 14b exhibited the most potent inhibitory activity against VEGFR-2 with IC50 value of 0.016 ± 0.002 μM and it showed the most potent antiproliferative effect against Hep-G2 and MCF-7 with IC50 values at low-micromolar range. Molecular docking studies revealed that these compounds represented by the most potent compound 14b could bind well to the ATP-binding site of VEGFR-2, which suggested that compound 14b could be a potential anticancer agent targeting VEGFR-2.
INFLUENZA VIRUS INHIBITOR TARGETING NUCLEOPROTEIN
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Paragraph 0102; 0105, (2019/06/09)
This document discloses a novel class of compound for treating influenza A and influenza B viral infection, and compositions and methods of use thereof.
Broad Spectrum Inhibitor of Influenza A and B Viruses Targeting the Viral Nucleoprotein
White, Kris M.,Abreu, Pablo,Wang, Hui,De Jesus, Paul D.,Manicassamy, Balaji,García-Sastre, Adolfo,Chanda, Sumit K.,Devita, Robert J.,Shaw, Megan L.
, p. 146 - 157 (2018/02/14)
S119 was a top hit from an ultrahigh throughput screen performed to identify novel inhibitors of influenza virus replication. It showed a potent antiviral effect (50% inhibitory concentration, IC50 = 20 nM) and no detectable cytotoxicity (50% c
Pharmaceutical compositions containing phenylamides
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, (2008/06/13)
Pharmaceutical compositions for inhibiting the aggregation of erthyrocytes or thrombocytes which include phenylamides which conform to the formula: STR1 with R1-6, X, A and B being as defined. Processes for the preparation of novel phenylamides
