查尔酮-苯并硼氧杂环戊烷杂化物作为新型抗癌剂。
Chalcone-benzoxaborole hybrids as novel anticancer agents.
作者信息
Zhang Jiong, Yang Fei, Qiao Zhitao, Zhu Mingyan, Zhou Huchen
机构信息
State Key Laboratory of Microbial Metabolism, School of Pharmacy, Shanghai Jiao Tong University, Shanghai, China.
State Key Laboratory of Microbial Metabolism, School of Pharmacy, Shanghai Jiao Tong University, Shanghai, China; Chemical Biology Division of Shanghai Universities E-Institutes, Key Laboratory of Cell Differentiation and Apoptosis of Chinese Ministry of Education, Shanghai Jiao Tong University School of Medicine, Shanghai, China.
出版信息
Bioorg Med Chem Lett. 2016 Dec 1;26(23):5797-5801. doi: 10.1016/j.bmcl.2016.10.024. Epub 2016 Oct 12.
In this study, we report the synthesis of a series of chalcone-benzoxaborole hybrid molecules and the evaluation of their anticancer activity. Their anticancer potency and toxicity were tested on three human cancer cell lines and two normal cell lines. The 4-fluoro compound 15 was found to be the most potent compound with an IC value of 1.4μM on SKOV3 cells. The 4-iodo compound 18 and 3-methyloxy-4-amino compound 47 showed good potency on SKOV3 cells while exhibiting low toxicity on normal cells. This work extended the application of benzoxaboroles to the field of anticancer research.
在本研究中，我们报道了一系列查尔酮-苯并硼氧杂环戊烷杂化分子的合成及其抗癌活性评估。在三种人类癌细胞系和两种正常细胞系上测试了它们的抗癌效力和毒性。发现4-氟化合物15是最有效的化合物，对SKOV3细胞的IC值为1.4μM。4-碘化合物18和3-甲氧基-4-氨基化合物47对SKOV3细胞显示出良好的效力，同时对正常细胞表现出低毒性。这项工作将苯并硼氧杂环戊烷的应用扩展到了抗癌研究领域。
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