Abstract
AbstractA 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.
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