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Described herein is a facile and efficient methodology toward the synthesis of novel convolutamydine A-incorporated morusignin L scaffold 3 from an Aldol addition event of carbonyl compounds to isatins via enamine catalysis. Products featuring a quaternary carbon center were smoothly obtained in good yields (up to 85% yield). This protocol also represents the first construction of flavonoid skeleton fused oxindole molecules, thus leading to new knowledge in the fields of both molecular complexity and diversity synthesis and the lead compound discovery. Furthermore, their biological activities against human prostate cancer cells PC-3 and human leukemia cells K562 have been preliminarily demonstrated by in vitro assays. The results demonstrated that most of these compounds obtained by this protocol showed comparable or even much better activity than the positive control of Cisplatin.