Article

Design, synthesis and biological evaluation of novel chalcone derivatives as antitubulin agents.

State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210093, PR China.
Bioorganic & medicinal chemistry (impact factor: 2.82). 04/2012; 20(10):3212-8. DOI:10.1016/j.bmc.2012.03.055 pp.3212-8
Source: PubMed

ABSTRACT A series of novel chalcone derivatives have been designed and synthesized, and their biological activities were also evaluated as potential inhibitors of tubulin. These compounds were assayed for growth-inhibitory activity against MCF-7 and A549 cell lines in vitro. Compound 3d showed the most potent antiproliferative activity against MCF-7 and A549 cell lines with IC(50) values of 0.03 and 0.95 μg/mL and exhibited the most potent tubulin inhibitory activity with IC(50) of 1.42 μg/mL. Docking simulation was performed to insert compound 3d into the crystal structure of tubulin at colchicines binding site to determine the probable binding model. Based on the preliminary results, compound 3d with potent inhibitory activity in tumor growth may be a potential anticancer agent.

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Keywords

A549 cell lines
 
colchicines binding site
 
Compound 3d
 
crystal structure
 
growth-inhibitory activity
 
novel chalcone derivatives
 
potent antiproliferative activity
 
potent inhibitory activity
 
potent tubulin inhibitory activity
 
potential anticancer agent
 
potential inhibitors
 
preliminary results
 
probable binding model
 
vitro
 

Hui Zhang