期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 27, 期 15, 页码 3326-3331出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2017.06.019
关键词
Indolin-2-one; Privileged structure; Cytotoxicity; Molecular mechanism
资金
- National Natural Science Foundation of China [81172985, 81261120391]
- CAMS Innovation Fund for Medical Sciences (CIFMS) [2016-I2M-3-009]
- NIH Grant from the National Cancer Institute [CA177584]
- Eshelman Institute for Innovation, Chapel Hill, North Carolina
The indolin-2-one core is a privileged structure for antitumor agents, especially kinase inhibitors. Twenty-three novel indolin-2-ones were designed by molecular dissection of the anticancer drug indirubin. Seventeen of them exhibited significant inhibition against the tested cell lines, and two of them (1c and 1h) showed IC50 values at the submicromolar level against HCT-116 cells. Compounds 1c and 2c were also potent inhibitors of the triple-negative breast cancer (TNBC) cell line MDA-MB-231. Flow cytometry was utilized to explore the antitumor mechanism of 1c and 2c with MDA-MB-231 cells, and distinct effects were observed on 2c. Furthermore, immunocytochemical examination of 1c suggested a destabilization of microtubules, which was significantly different from the effect of IM, an indirubin derivative. (C) 2017 Elsevier Ltd. All rights reserved.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据