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http://dx.doi.org/10.5012/bkcs.2013.34.8.2480

Synthesis and Preliminary Cytotoxicity Evaluation of New Diarylamides and Diarylureas Possessing 2,3-Dihydropyrrolo[3,2-b]quinoline Scaffold  

Kim, Hyun-Jin (Center for Biomaterials, Korea Institute of Science and Technology)
El-Gamal, Mohammed I. (Center for Biomaterials, Korea Institute of Science and Technology)
Lee, Yong Sup (Department of Pharmaceutical Science, College of Pharmacy & Department of Life and Nanopharmaceutical Science, Kyung Hee University)
Oh, Chang-Hyun (Center for Biomaterials, Korea Institute of Science and Technology)
Publication Information
Abstract
A new series of diarylamides and diarylureas having 2,3-dihydropyrrolo[3,2-b]quinoline scaffold was synthesized. Their in vitro antiproliferative activities were tested over NCI-60 cancer cell lines of nine different cancer types. Some target compounds showed good inhibition percentages over different cell lines. Among all the target compounds, compound 1f possessing 6,7-dimethoxy-2,3-dihydropyrrolo[3,2-b]quinoline nucleus, amide linker, and 4-chloro-3-(trifluoromethyl)phenyl terminal ring showed high selectivity against MCF7 and MDA-MB-468 breast cancer cell lines more than the other tested cell lines. Its inhibition percentages at $10{\mu}M$ concentration over those two cell lines were 84.97% and 87.13%, respectively.
Keywords
2,3-Dihydropyrrolo[3,2-b]quinoline; Urea; Amide; Antiproliferative activity; Breast cancer;
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