A diastereoselective three-component reaction for the assembly of succinimide and isatin hybrid molecules with potent anticancer activities

A Rh-2(OAc)(4) catalyzed three-component reaction of vinyl diazosuccinimides with alcohols and isatins has been reported, which provides a practical assess to the direct assembly of succinimide and isatin hybrid molecules in good-to-high yields with excellent stereoselectivity. The antiproliferation activity of these synthesized succinimide and isatin hybrid products has been tested via the CCK8 assay in different cancer cell lines, and compounds 4g (SJSA-1, IC50 = 3.82 mu M) and 4r (HCT-116, IC50 = 9.02 mu M) exhibit higher anticancer potency than other tested compounds. [GRAPHICS] .

Automated summary

A Rh-2(OAc)(4) catalyzed three-component reaction enables the direct assembly of succinimide and isatin hybrid molecules with good-to-high yields and excellent stereoselectivity. The synthesized products exhibit significant anticancer potency, especially compounds 4g and 4r.