Abstract
New series of pyrimido[4,5-b]quinolines and [1,2,4]triazolo[2′,3′:3,4]pyrimido[6,5-b]quinolines have been synthesized. Compounds 4a, 4e, 4f, 4h, 5b, 5d, 6a, 6d, 6e, 8c, 8d, 10c–e, 10h, 11a, 11b, and 12a were tested for in vitro antitumor activity against human breast carcinoma (MCF-7) cell line, where compound 8d was found to be the most active member with IC50 value of 3.62 μM. The DNA-binding affinity for the same compounds showed that compounds 8d and 10d exhibited the highest affinity to DNA. The detailed synthesis, spectroscopic, and biological data are reported.
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Acknowledgments
The authors would like to express their sincere thanks to Prof. Dr. Farid A. Badria, Pharmacognosy Department, Faculty of Pharmacy, Mansoura University, Egypt, for carrying out the DNA-binding assay, and to all members of Pharmacology Unit at the National Cancer Institute (NCI), Cairo University, for performing the cytotoxicity testing.
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El-Ashmawy, M.B., El-Sherbeny, M.A. & El-Gohary, N.S. Synthesis and antitumor screening of new series of pyrimido-[4,5-b]quinolines and [1,2,4]triazolo[2′,3′:3,4]pyrimido[6,5-b]quinolines. Med Chem Res 22, 2724–2736 (2013). https://doi.org/10.1007/s00044-012-0272-y
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DOI: https://doi.org/10.1007/s00044-012-0272-y