4.4 Article

Quinoline Consists of 1H-1,2,3-Triazole Hybrids: Design, Synthesis and Anticancer Evaluation

期刊

CHEMISTRYSELECT
卷 4, 期 48, 页码 14184-14190

出版社

WILEY-V C H VERLAG GMBH
DOI: 10.1002/slct.201903938

关键词

Anticancer Evaluation; CuAAC strategy; Quinoline; Suzuki coupling; triazoles

资金

  1. Science and Engineering Research Board-Department of Science and Technology (SERB-DST), New Delhi, India [EMR/2016/001411]

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A series of novel 8-bromo-1H-1,2,3-triazol-4-yl-2-methylquinoline derivatives and their Suzuki coupling products were synthesized via Copper catalyzed azide-alkyne cycloaddition (CuAAC) strategy followed by microwave assisted Suzuki coupling for the development of new series of anticancer agents. The invitro anticancer activity of the synthesized compounds were screened against human breast cancer (MDA-MB-231) and melanoma cell lines (B16F10). Among these, compounds 5 c (Azetidine), 5 e (Nitro benzoate), 5 f (fluorobenzyl)-1H-pyrazole), 5 g (Boc piperidine), 6 a (cyclo propyl), 6 c (5-fluoro-6-methoxypyridin-3-yl)and 6 d (2-methoxypyridin-3-yl) were showed anticancer activity ranging from 13.44 mu M to 38.2 mu M. The cellular toxicity of the novel compounds was also evaluated using normal human embryonic kidney (HEK) cell lines.

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