2. Academic Validation
  3. Enmein-type diterpenoid analogs from natural kaurene-type oridonin: Synthesis and their antitumor biological evaluation

Enmein-type diterpenoid analogs from natural kaurene-type oridonin: Synthesis and their antitumor biological evaluation

  • Eur J Med Chem. 2013 Jun:64:215-21. doi: 10.1016/j.ejmech.2013.04.012.
Dahong Li 1,  Shengtao Xu,  Hao Cai,  Lingling Pei,  Hengyuan Zhang,  Lei Wang,  Hequan Yao,  Xiaoming Wu,  Jieyun Jiang,  Yijun Sun,  Jinyi Xu
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, China.
PMID: 23644204 DOI: 10.1016/j.ejmech.2013.04.012
Abstract

A series of enmein-type diterpenoid analogs (11-20) derived from natural kaurene-type diterpenoid oridonin were synthesized and biologically evaluated. All target compounds showed improved anti-proliferative activities against four human Cancer cell lines compared with natural oridonin and parent compound 10. Some compounds were more potent than positive control Taxol. Furthermore, mechanistic investigation showed that the representative compound 17 affected cell cycle and induced Apoptosis at low micro-molar level in human hepatoma Bel-7402 cells, via an oxidative stress triggered mitochondria-related caspase-dependent pathway.

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