Mohareb Rafat M, MegallyAbdo Nadia Y
Chemistry Department, Faculty of Science, Cairo University, Giza 12613, Egypt.
Chemistry Department, Faculty of Education, Alexandria University, Alexandria 21526, Egypt.
Molecules. 2015 Jun 23;20(6):11535-53. doi: 10.3390/molecules200611535.
In this work, 3-bromoacetylcoumarin was used as the key starting material for the synthesis of pyran, pyridine, thiophene, thiazole and pyrazole derivatives through its reaction with different reagents. The structures of the newly synthesized compounds were confirmed on the basis of their spectral data and elemental analyses. All of the synthesized compounds were screened for their in vitro anticancer activity against six human cancer cell lines, namely: human gastric cancer (NUGC), human colon cancer (DLD1), human liver cancer (HA22T and HEPG2), nasopharyngeal carcinoma (HONE1), human breast cancer (MCF) and normal fibroblast cells (WI38). The IC50 values (the sample concentration that produces 50% reduction in cell growth) in nanomolars (nM)) showed most of the compounds exhibited significant cytotoxic effect. Among these derivatives, compound 6d showed almost equipotent cytotoxic activity against NUGC (IC50 = 29 nM) compared to the standard CHS 828 (IC50 = 25 nM).
在本研究中，3-溴乙酰香豆素被用作关键起始原料，通过与不同试剂反应合成吡喃、吡啶、噻吩、噻唑和吡唑衍生物。新合成化合物的结构通过光谱数据和元素分析得以确证。对所有合成化合物针对六种人类癌细胞系进行了体外抗癌活性筛选，这六种细胞系分别为：人类胃癌细胞系（NUGC）、人类结肠癌细胞系（DLD1）、人类肝癌细胞系（HA22T和HEPG2）、鼻咽癌细胞系（HONE1）、人类乳腺癌细胞系（MCF）以及正常成纤维细胞系（WI38）。以纳摩尔（nM）为单位的半数抑制浓度（IC50）值（即导致细胞生长降低50%的样品浓度）表明，大多数化合物表现出显著的细胞毒性作用。在这些衍生物中，与标准品CHS 828（IC50 = 25 nM）相比，化合物6d对NUGC显示出几乎相当的细胞毒性活性（IC50 = 29 nM）。
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