【摘 要】
：
A series of novel spirolactone-type diterpenoid derivatives of oridonin (12a-j) were designed and synthesized.All the compounds showed significant anti-proliferative activity against a panel of human
【机 构】
：
Department of Medicinal Chemistry;State Key Laboratory of Natural Medicines,China Pharmaceutical Uni
【出 处】
：
第九届IUPAC化学生物学国际研讨会暨第八届世界华人药物化学研讨会
论文部分内容阅读
A series of novel spirolactone-type diterpenoid derivatives of oridonin (12a-j) were designed and synthesized.All the compounds showed significant anti-proliferative activity against a panel of human tumor cell lines and the most cytotoxic compound 12j was more potent than positive control Taxol in K562 and Bel-7402 cells with IC50 values of 0.39μM and 1.39μM,respectively.Furthermore,the cellular mechanism of action of these compounds,including induction of early and late stage apoptosis and significant increase of cell population in the G2/M phase at low micromolar concentrations on human hepatoma Bel-7402 cells were first presented.
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