Type

Journal Article

Authors

Peter T.M. Kenny
Blánaid White
John Crown
Norma O'Donovan
Thamir Maghoub
Rachel Tiedt
Aine Mooney

Subjects

Chemistry

Topics
dna damage cell cycle antineoplastic agents chemistry coordination complexes esters drug screening assays antitumor ferrocene cell proliferation drug effects ferrous compounds naphthalenes cell line tumor guanine dipeptides pharmacology chemical synthesis oxidation reduction humans structure activity relationship

Structure--activity relationship and mode of action of N-(6-ferrocenyl-2-naphthoyl) dipeptide ethyl esters: novel organometallic anticancer compounds. (2012)

Abstract 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 IC(50) values of 0.13 and 0.14 μM, respectively. These compounds were also found to have significant activity in the Sk-Mel-28 malignant melanoma cell line (IC(50) values of 1.10 and 1.06 μM, 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.
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Full list of authors on original publication

Peter T.M. Kenny, Blánaid White, John Crown, Norma O'Donovan, Thamir Maghoub, Rachel Tiedt, Aine Mooney

Experts in our system

1
Peter T.M. Kenny
Dublin City University
Total Publications: 20
 
2
Blánaid White
Dublin City University
Total Publications: 24
 
3
John Crown
Dublin City University
Total Publications: 104
 
4
Norma O'Donovan
Dublin City University
Total Publications: 59