Synthesis and evaluation of cytotoxic effects of novel α-methylenelactone tetracyclic diterpenoids.

Abstract

A series of tetracyclic diterpenoids bearing the α-methylenelactone group have been synthesized and screened for their in vitro anti-tumor activities against six human cancer cell lines. The results showed that compounds 1c, 2a and 2b exhibited significant cytotoxicity superior to the positive control doxorubicin hydrochloride against MDA-MB-231, K562 and HepG2 cell lines. In particular, compound 2b was identified as the most promising anticancer agent against HepG2 cells with IC(50) value of 0.09μM.

• Authors: Yao-Fu Zeng, Jia-Qiang Wu, Lian-Yong Shi, Ke Wang, Bin Zhou, Yong Tang, Da-Yong Zhang, Yang-Chang Wu, Wei-Yi Hua, Xiao-Ming Wu
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 22 Issue 5 Pg. 1922-5 (Mar 01 2012) ISSN: 1464-3405 [Electronic] England
• PMID: 22318158 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2012 Elsevier Ltd. All rights reserved.

Chemical References

• Antineoplastic Agents
• Diterpenes
• Lactones
• methylene-lactone

Topics

• Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
• Cell Line, Tumor
• Cell Survival (drug effects)
• Diterpenes (chemical synthesis, chemistry, pharmacology)
• Humans
• Lactones (chemical synthesis, chemistry, pharmacology)
• Neoplasms (drug therapy)
• Structure-Activity Relationship