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.
Molecules. 2019 Apr 18;24(8):1529. doi: 10.3390/molecules24081529.
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 (H- and, C-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 (, , , , ) 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.
我们之前的研究结果表明，苯并呋喃的某些衍生物，特别是卤代衍生物，对人类白血病细胞具有选择性毒性。在继续研究这组化合物的过程中，我们在此报告了关于 14 种新的苯并呋喃衍生物的合成以及物理化学和生物学特性的新数据，其中包括 6 种溴代化合物。所有新化合物的结构均通过光谱方法（H-和 C-NMR、ESI MS）和元素分析确定。评估了它们对 K562（白血病）、MOLT-4（白血病）、HeLa（宫颈癌）和正常细胞（HUVEC）的细胞毒性。五种化合物（、、、、）对所有测试的细胞系均显示出显著的细胞毒性活性，并对癌细胞系具有选择性。SAR 分析（结构-活性关系分析）表明，引入到苯并呋喃系统上的甲基或乙酰基的溴取代增加了它们在正常和癌细胞中的细胞毒性。
