Synthesis and Anti-human Leukemia Cells Activity of Novel Bispiro-pyrrolidone-oxindole-hexahydroxanthone Hybrids
The synthesis of a diverse derivative library of natural product-derived privileged backbones is an important topic in the field of plant chemistry.In this paper,based on a new methodological strategy,we uses oxindole-chromone synthon(1)and 3-en-2-carbonyl pyrrolidine(2)as starting materi-als,the reaction undergoes a[4+2]cycloaddition reaction to provide ten bispiro-pentolactam-oxin-dole-hexahydroxanthone hybrids 3a～3j in 73％～85％yields and dr>20/1.The structures of prod-ucts 3 were characterized by 1H NMR,13C NMR and HR-MS(ESI-TOF).The relative configuration of compound 3j was further determined by single crystal X-ray diffraction.The in vitro antitumor activities against human leukemia cells(K562)were demonstrated by MTT.The results showed that bispiro-pen-tolactam-oxindole-hexahydroxanthone hybrids 3b,3e,3g and 3i showed good cytotoxic effects on K562.
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