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

  • Bioorg Med Chem Lett. 2012 Mar 1;22(5):1922-5. doi: 10.1016/j.bmcl.2012.01.051.
Yao-Fu Zeng  1 ,  Jia-Qiang Wu ,  Lian-Yong Shi ,  Ke Wang ,  Bin Zhou ,  Yong Tang ,  Da-Yong Zhang ,  Yang-Chang Wu ,  Wei-Yi Hua ,  Xiao-Ming Wu
Affiliations
  • 1. Center of Drug Discovery, College of Pharmacy, China Pharmaceutical University, 24 Road Tongjia Xiang, Nanjing 210009, China.
PMID: 22318158 DOI: 10.1016/j.bmcl.2012.01.051
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.