Bin-bin Song, Zi-kuo Zhang, Qing-feng Zhu, Gu He, Ju-zheng Fan
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[Design, synthesis and evaluation of a novel MEK protein inhibitors].
This study was conducted to design and synthetize highly efficient, specific, non-resistant
small MEK inhibitors. Based on active small molecules which have been reported, we studied the action
mode with MEK protein using Autodock 4.2, generated innovative and feasible design method, designed
novel small MEK protein inhibitors with a reference to molecular modeling and docking. The anti-tumor
activities of four kinds of cells including MCF-7, PANC-1, SY5Y, A549 were tested with MTT method
in vitro. The structure of 10 new small molecules has been determined with 1H NMR and 13C NMR. The
compounds 4, 6, 7, 8, 10 had high antitumor activities, the compounds 1, 3, 5 also showed good activity,
and the compounds 2, 9 showed cell selectivity in killing tumor.
药学学报Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (all)
CiteScore
1.20
自引率
0.00%
发文量
0
期刊介绍:
Acta Pharmaceutica Sinica B (APSB) is a bimonthly English peer-reviewed online journal in ScienceDirect, which publishes significant original research articles, communications and high quality reviews of recent advances. APSB encourages submissions from all areas of pharmaceutical sciences, including pharmacology, pharmaceutics, medicinal chemistry, natural products, pharmacognosy, pharmaceutical analysis and pharmacokinetics.
APSB is a part of the series Acta Pharmaceutica Sinica, which was founded in 1953. The journal is co-published by Elsevier B.V., in association with the Institute of MateriaMedica, Chinese Academy of Medical Sciences and Chinese Pharmaceutical Association.