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

Medicinal Chemistry Research
2013.0

Abstract

New series of pyrimido[4,5-b]quinolines and [1,2,4]triazolo[20 ,30 :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 lM. 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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