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[摘要]：Quinoline derivatives posses many types of biological activities and have been reported to show significant anticancer activity. There is a variety of mechanisms for the anticancer activity and the most distinguished mechanism is the inhibition of vascular epithelial growth factor receptor tyrosine kinase (VEGFRTK). Novel quinoline derivatives 6-12 and pyrimido[4,5-b]quinoline derivatives 16-20 are reported herein. All the newly synthesized compounds were evaluated for their in vitro anticancer activity against human breast cancer cell line (MCF7) in which VEGFR is highly expressed. Compounds 6 and 7 with IC(50) values of 8.5 mu M and 21.9 mu M were the most active compounds and exhibited cytotoxic activities higher than that of the reference drug doxorubicin (IC(50) = 32.02 mu M). The most active compounds 6 and 7 were further evaluated for their ability to enhance the cell killing effect of c-radiation. |
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