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Design and synthesis of some novel quinoline derivatives as anticancer and radiosensitizing agents targeting VEGFR tyrosine kinase
Author(s) -
Ghorab Mostafa M.,
Ragab Fatma A.,
Heiba Helmy I.,
Ghorab Walid M.
Publication year - 2011
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.749
Subject(s) - chemistry , quinoline , doxorubicin , tyrosine kinase , pharmacology , tyrosine kinase inhibitor , cell culture , in vitro , receptor tyrosine kinase , cytotoxic t cell , kinase , cancer research , biochemistry , cancer , receptor , chemotherapy , organic chemistry , biology , genetics
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).