Shan, Yuanyuan published the artcileDiscovery of novel VEGFR-2 inhibitors. Exploration of diverse hinge-binding fragments via core-refining approach, Recommanded Product: 1H-Pyrazole-4-boronic acid, the publication is European Journal of Medicinal Chemistry (2015), 80-90, database is CAplus and MEDLINE.
Pathol. angiogenesis plays a critical role in numerous diseases including malignancy. VEGFR-2 is the central regulators in angiogenesis and has become a promising target for anticancer drug design. The authors have identified a novel biphenyl-aryl urea incorporated with salicyladoxime (BPS-7) as potent VEGFR-2 inhibitor. As a continuation to the previous research, various aromatic-heterocyclic were introduced as hinge-binding fragment via a core-refining approach. Interestingly, many compounds exhibited comparable VEGFR-2 inhibition to Sorafenib. In particular, I and II displayed excellent VEGFR-2 inhibitory activity with IC50 values of 0.50 nM and 0.79 nM, resp. Several title compounds showed considerable antiproliferative activity against A549 and SMMC-7721 cells. In addition, mol. docking was performed to rationalize the efficiency of the better compounds These results will be instructive for further inhibitor design and optimization.
European Journal of Medicinal Chemistry published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C27H39ClN2, Recommanded Product: 1H-Pyrazole-4-boronic acid.
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