摘要
A novel series of 3-pyrrolo[b]cyclohexylene-2-dihydroindolinone derivatives targeting VEGFR-2, PDGFR-β and c-Kit kinases were designed and synthesized. The molecular design was based on the SAR features of indolin-2-ones as kinase inhibitors. SAR study of the series allowed us to identify compounds possessing more potent inhibitory activities against the three kinases than sunitinb with IC50 values in the low nanomolar range in vitro. Additionally, some compounds also showed favorable antiproliferative activities against a panel of cancer cell lines (BXPC-3, T24, BGC, HEPG2 and HT29).
| 源语言 | 英语 |
|---|---|
| 页（从-至） | 5630-5633 |
| 页数 | 4 |
| 期刊 | Bioorganic and Medicinal Chemistry Letters |
| 卷 | 23 |
| 期 | 20 |
| DOI | |
| 出版状态 | 已出版 - 15 10月 2013 |
指纹
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Ding, L., Tang, F., Huang, W., Jin, Q., Shen, H., & Wei, P. (2013). Design, synthesis, and biological evaluation of novel 3-pyrrolo[b] cyclohexylene-2-dihydroindolinone derivatives as potent receptor tyrosine kinase inhibitors. Bioorganic and Medicinal Chemistry Letters, 23(20), 5630-5633. https://doi.org/10.1016/j.bmcl.2013.08.037