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Open AccessArticle

Synthesis of New Derivatives of Benzofuran as Potential Anticancer Agents

Chair and Department of Biochemistry, Medical University of Warsaw, 1 Banacha Str., 02-097 Warsaw, Poland
Centre of Molecular and Macromolecular Studies, Polish Academy of Sciences, 112 Sienkiewicza Str., 90-363 Łódź, Poland
Authors to whom correspondence should be addressed.
Academic Editor: Qiao-Hong Chen
Molecules 2019, 24(8), 1529;
Received: 28 March 2019 / Revised: 15 April 2019 / Accepted: 16 April 2019 / Published: 18 April 2019
(This article belongs to the Special Issue Anticancer Agents: Design, Synthesis and Evaluation)
The results of our previous research indicated that some derivatives of benzofurans, particularly halogeno-derivatives, are selectively toxic towards human leukemia cells. Continuing our work with this group of compounds we here report new data on the synthesis as well as regarding the physico-chemical and biological characterization of fourteen new derivatives of benzofurans, including six brominated compounds. The structures of all new compounds were established by spectroscopic methods (1H- and, 13C-NMR, ESI MS), and elemental analyses. Their cytotoxicity was evaluated against K562 (leukemia), MOLT-4 (leukemia), HeLa (cervix carcinoma), and normal cells (HUVEC). Five compounds (1c, 1e, 2d, 3a, 3d) showed significant cytotoxic activity against all tested cell lines and selectivity for cancer cell lines. The SAR analysis (structure-activity relationship analysis) indicated that the presence of bromine introduced to a methyl or acetyl group that was attached to the benzofuran system increased their cytotoxicity both in normal and cancer cells. View Full-Text
Keywords: benzofurans; chemical synthesis; cytotoxic properties; HeLa; MOLT-4; K562 benzofurans; chemical synthesis; cytotoxic properties; HeLa; MOLT-4; K562
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MDPI and ACS Style

Napiórkowska, M.; Cieślak, M.; Kaźmierczak-Barańska, J.; Królewska-Golińska, K.; Nawrot, B. Synthesis of New Derivatives of Benzofuran as Potential Anticancer Agents. Molecules 2019, 24, 1529.

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