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

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.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Mooney A,Tiedt R,Maghoub T,O'Donovan N,Crown J,White B,Kenny PT

doi

10.1021/jm3004027

subject

Has Abstract

pub_date

2012-06-14 00:00:00

pages

5455-66

issue

11

eissn

0022-2623

issn

1520-4804

journal_volume

55

pub_type

杂志文章

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