2. Academic Validation
  3. Synthesis and evaluation of cytotoxic effects of novel α-methylenelactone tetracyclic diterpenoids

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

Affiliation

  • 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.

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