Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 27, Issue 15, Pages 3326-3331Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2017.06.019
Keywords
Indolin-2-one; Privileged structure; Cytotoxicity; Molecular mechanism
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Funding
- 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
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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.
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