Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 21, Issue 7, Pages 1724-1734Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2013.01.047
Keywords
RSK2; Kinase inhibitor; Molecular docking
Funding
- Fundamental Research Funds for the Central Universities
- National Natural Science Foundation of China [21173076, 81102375, 10979072, 81230090, 81222046, 81230076]
- Special Fund for Major State Basic Research Project [2009CB918501]
- Shanghai Committee of Science and Technology [09dZ1975700, 11DZ2260600, 10431902600]
- 863 Hi-Tech Program of China [2012AA020308]
- National S&T Major Project of China [2011ZX09307-002-03]
- Program for New Century Excellent Talents in University [NCET-10-0378]
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A series of novel indolin-2-ones inhibitors against p90 ribosomal S6 protein kinase 2 (RSK2) were designed and synthesized and their structure-activity relationship (SAR) was studied. The most potent inhibitor, compound 3s, exhibited potent inhibition against RSK2 with an IC50 value of 0.5 mu M and presented a satisfactory selectivity against 23 kinases. The interactions of these inhibitors with RSK2 were investigated based on the proposed binding poses with molecular, docking simulation. Four compounds and six compounds exhibited moderate anti-proliferation activities against PC 3 cells and MCF-7 cells, respectively. (C) 2013 Elsevier Ltd. All rights reserved.
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