Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 55, Issue 11, Pages 5455-5466Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm3004027
Keywords
-
Categories
Funding
- Embark Initiative
- IRCSET
- Health Research Board [HRA/09/86]
Ask authors/readers for more resources
In this article, we report the findings of a comprehensive structure-activity relationship study of N-(6-ferrocenyl-2-naphthoyl) dipeptide ethyl esters, in which novel analogues were designed, synthesized, and evaluated in vitro for antiproliferative effect. Two new compounds, 2 and 16, showed potent nanomolar activity in the H1299 NSCLC cell line, with exceptional IC50 values of 0.13 and 0.14 mu M, respectively. These compounds were also found to have significant activity in the Sk-Mel-28 malignant melanoma cell line (IC50 values of 1.10 and 1.06 mu M, respectively). Studies were also conducted to elucidate the mode of action of these novel organometallic anticancer compounds. Cell cycle analysis in the H1299 cell line suggests these compounds induce apoptosis, while guanine oxidation studies confirm that 2 is capable of generating oxidative damage via a ROS-mediated mechanism.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available