Design and synthesis of some novel quinoline derivatives as anticancer and radiosensitizing agents targeting VEGFR tyrosine kinase

✍ Scribed by Mostafa M. Ghorab; Fatma A. Ragab; Helmy I. Heiba; Walid M. Ghorab

• Publisher: Journal of Heterocyclic Chemistry
• Year: 2011
• Tongue: English
• Weight: 832 KB
• Volume: 48
• Category: Article
• ISSN: 0022-152X
• DOI: 10.1002/jhet.749

✦ Synopsis

Abstract

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, 7a, 7b, 7c, 8, 9, 10, 11, 12 and pyrimido[4,5‐b]quinoline derivatives 16, 17, 18, 19, 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 μ__M__ and 21.9 μ__M__ were the most active compounds and exhibited cytotoxic activities higher than that of the reference drug doxorubicin (IC~50~= 32.02 μ__M__). The most active compounds 6 and 7 were further evaluated for their ability to enhance the cell killing effect of γ‐radiation. J. Heterocyclic Chem., (2011).