Design, synthesis and evaluation of a novel MEK protein inhibitors
10.16438/j.0513-4870.2016-0926
- VernacularTitle:MEK小分子抑制剂的设计、合成与初步活性研究
- Author:
Bin-bin SONG
1
;
Zi-kuo ZHANG
1
;
Qing-feng ZHU
1
;
Gu HE
2
;
Ju-zheng FAN
1
Author Information
1. West China School of Pharmacy, Sichuan University, Chengdu 610041, China
2. State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu 610041, China
- Publication Type:ORIGINAL ARTICLES
- Keywords:
MEK;
design;
synthesize;
anti-tumor activity
- From:
Acta Pharmaceutica Sinica
2017;52(3):416-424
- CountryChina
- Language:Chinese
-
Abstract:
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.
