Benzofuran-isatin conjugates as potent VEGFR-2 and cancer cell growth inhibitors |
| |
Authors: | Yulin Zou |
| |
Affiliation: | The Third Clinical Medical College of the Three Gorges University, Gezhouba Central Hospital of Sinopharm, Yichang, 443002 Hubei, China |
| |
Abstract: | A series of benzofuran-isatin conjugates 6a-l and 7a,b tethered by various alkyl linkers were synthesized and evaluated for their VEGFR-2 inhibitory activity and in vitro activity against a panel of cancer cell lines. Seven of them were comparable with or better than Sunitinib against all tested cancer cells, demonstrating benzofuran-isatin conjugates were potential anticancer candidates. The mechanism study revealed that VEGFR-2 was at least one of the targets for this kind of conjugates. The structure-activity relationship demonstrated that the carbon spacer between benzofuran and isatin moieties, substituents on the C-2 position of benzofuran moiety, and substituents on C-3 as well as C-5 position of isatin motif influenced the anticancer activity significantly, and the enriched structure-activity relationship may provide an insight for rational design of more effective conjugates. |
| |
Keywords: | |
|
|