4.2 Article

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

Journal

MEDICINAL CHEMISTRY RESEARCH
Volume 22, Issue 6, Pages 2724-2736

Publisher

SPRINGER BIRKHAUSER
DOI: 10.1007/s00044-012-0272-y

Keywords

Pyrimido[4,5-b]quinolines; [1,2,4]Triazolo[2 ' 3 ':3,4]pyrimido[6,5-b]quinolines; In vitro antitumor screening

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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 mu M. 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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