原创力文档discovery of indolin-2-one derivatives as potent pak4 inhibitors structure-activity relationship analysis, biological evaluation and molecular docking study：（发现indolin-2-one衍生品作为强有力的pak4抑制剂的构效关系分析,生物评价和分子对接研究）.pdfVIP
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discovery of indolin-2-one derivatives as potent pak4 inhibitors structure-activity relationship analysis, biological evaluation and molecular docking study：（发现indolin-2-one衍生品作为强有力的pak4抑制剂的构效关系分析,生物评价和分子对接研究）
Bioorganic Medicinal Chemistry 25 (2017) 3500–3511
Contents lists available at ScienceDirect
Bioorganic Medicinal Chemistry
journal homepage: www.else /locate/bmc
Discovery of indolin-2-one derivatives as potent PAK4 inhibitors:
Structure-activity relationship analysis, biological evaluation and
molecular docking study
Jing Guo a, Mingyue Zhu a, Tianxiao Wu a, Chenzhou Hao a, Kai Wang a, Zizheng Yan a, Wanxu Huang a,b,
Jian Wang a, Dongmei Zhao a,⇑, Maosheng Cheng a,⇑
a Key Laboratory of Structure-Based Drug Design Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, PR China
b School of Life Science and Bio-pharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, PR China
a r t i c l e i n f o a b s t r a c t
Article history: Utilizing a pharmacophore hybridization approach, a novel series of substituted indolin-2-one derivatives
Received 21 April 2017 were designed, synthesized and evaluated for their in vitro biological activities against p21-activated
Revised 26 April 2017 kinase 4. Compounds 11b, 12d and 12g exhibited the most potent inhibitory activity against PAK4
Accepted 28 April 2017
(IC50 = 22 nM, 16 nM and 27 nM, respectively). Among them, compound 12g showed the highest antipro-
Available online 3 May 2017
liferative activity against A549 cells (IC50 = 0.83 lM). Apoptosis analysis in A549 cells suggested that
compound 12g de
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