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

Bioorganic & medicinal chemistry letters (2012-02-10)
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
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.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Doxorubicin hydrochloride, suitable for fluorescence, 98.0-102.0% (HPLC)
Sigma-Aldrich
Doxorubicin hydrochloride, 98.0-102.0% (HPLC)