Design and Synthesis of Some Novel Quinoline Derivatives as Anticancer and Radiosensitizing Agents Targeting VEGFR Tyrosine Kinase

作者：Ghorab Mostafa M^*; Ragab Fatma A; Heiba Helmy I; Ghorab Walid M

来源：Journal of Heterocyclic Chemistry, 2011, 48(6): 1269-1279.

DOI：10.1002/jhet.749

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 IC50 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 (IC50 = 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.

• 出版日期2011-11