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目的设计、合成并筛选具有抗乳腺癌活性的查耳酮类化合物。方法利用Claisen-Schmidt羟醛缩合反应,合成了一系列的查耳酮类化合物,并通过MTT法测试化合物抗乳腺癌活性。结果合成了36个查耳酮类化合物,其结构均通过1H-NMR和13C-NMR进行了表征。初步生物活性结果表明大部分目标分子查耳酮对MCF-7有较强的抑制活性,对MDA-MB-231也展现出了中等的抑制活性,其中化合物27(IC50=11.3μmol·L?1)对MCF-7的抑制活性是他莫昔芬的1.5倍,同时这些查尔酮类化合物对正常细胞均没有毒性。结论本研究为开发具有抗乳腺癌活性的查耳酮类化合物提供了参考和依据。
Objective To design, synthesize and screen chalcone compounds with anti-breast cancer activity. Methods A series of chalcone compounds were synthesized by Claisen-Schmidt aldol condensation reaction. The compounds were tested for anti-breast cancer activity by MTT assay. Results 36 chalcone compounds were synthesized and their structures were characterized by 1H-NMR and 13C-NMR. Preliminary bioassay results showed that most of the target molecules, chalcone, had a strong inhibitory activity on MCF-7 and a moderate inhibitory activity on MDA-MB-231. Compound 27 (IC50 = 11.3 μmol·L -1 ) Had a 1.5-fold inhibitory activity against MCF-7 compared to tamoxifen, and none of these chalcones were toxic to normal cells. Conclusion This study provides a reference and basis for the development of chalcone compounds with anti-breast cancer activity.