当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Synthesis of spirolactone-type diterpenoid derivatives from kaurene-type oridonin with improved antiproliferative effects and their apoptosis-inducing activity in human hepatoma Bel-7402 cells.

Synthesis of spirolactone-type diterpenoid derivatives from kaurene-type oridonin with improved antiproliferative effects and their apoptosis-inducing activity in human hepatoma Bel-7402 cells.

Abstract：

:A series of novel spirolactone-type diterpenoid derivatives of oridonin (12a-j) were designed and synthesized. All the target compounds showed improved anti-proliferative activity against a panel of human cancer cell lines and the most effective compound 12j was more potent than positive control Taxol in K562 and Bel-7402 cells with IC(50) values of 0.39 μM and 1.39 μM, respectively. The cellular mechanisms showed that compound 12j induced apoptosis at low micromolar concentrations in human hepatoma Bel-7402 cells. These results demonstrate that the spirolactone-type diterpenoid derivatives of oridonin have optimized growth inhibitory activity against cancer cells and interesting apoptosis-inducing ability.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Li D,Cai H,Jiang B,Liu G,Wang Y,Wang L,Yao H,Wu X,Sun Y,Xu J

doi

10.1016/j.ejmech.2012.11.002

subject

Has Abstract

pub_date

2013-01-01 00:00:00

pages

322-8

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(12)00660-5

journal_volume

59

pub_type

杂志文章

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