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

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.
Authors	Dahong Li, Shengtao Xu, Hao Cai, Lingling Pei, Hengyuan Zhang, Lei Wang, Hequan Yao, Xiaoming Wu, Jieyun Jiang, Yijun Sun, Jinyi Xu
Journal	European journal of medicinal chemistry (Eur J Med Chem) Vol. 64 Pg. 215-21 (Jun 2013) ISSN: 1768-3254 [Electronic] France
PMID	23644204 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Copyright	Copyright © 2013 Elsevier Masson SAS. All rights reserved.
Chemical References	Antineoplastic Agents Diterpenes Diterpenes, Kaurane oridonin kaurene enmein
Topics	Antineoplastic Agents (chemical synthesis, chemistry, pharmacology) Apoptosis (drug effects) Cell Cycle (drug effects) Cell Line, Tumor Diterpenes (chemical synthesis, chemistry, pharmacology) Diterpenes, Kaurane (chemistry) Dose-Response Relationship, Drug Drug Screening Assays, Antitumor Humans Molecular Conformation Structure-Activity Relationship

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