查耳酮类化合物合成及抗乳腺癌活性研究

Synthesis of Chalcone Derivatives and Anti-breast Cancer Screening

关键词:  查耳酮  合成  抗乳腺癌活性

Key words:  chalcone  synthesis  anti-breast cancer activity

摘要:

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=11.3 μmol·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。

Abstract:

OBJECTIVE To design, synthesis, and screen of chalcone derivatives with anti-breast cancer activity. METHODS The series of chalcone were synthesized by Claisen-Schmidt aldol condensation reaction, and the anti-breast cancer activity was assessed by MTT. RESULTS Thity six chalcone compounds were synthesized. All the target compounds had been confirmed by ¹H-NMR and ¹³C-NMR spectra. The preliminary biological results showed that most of chalcone derivatives displayed significant antiproliferative effect on MCF-7 breast cancer cells, which also showed moderate inhibitory activity, against MDA-MB-231 cell lines; specifically, compound 27(IC₅₀=11.3 μmol·L^-1) showed about 1.5-fold potency of tamoxifen, against MCF-7 cell lines, and these chalcone derivatives were not toxic to normal cells. CONCLUSION This study provides information and basis for development of chalcone compounds with anti-breast cancer activity.