학술논문
StructureâActivityRelationship and Mode ofAction of N-(6-Ferrocenyl-2-naphthoyl) DipeptideEthyl Esters: Novel Organometallic Anticancer Compounds.
Document Type
Article
Author
Source
Subject
*STRUCTURE-activity relationship in pharmacology
*DIPEPTIDES
*ETHYL esters
*DRUG design
*ANTINEOPLASTIC agents
*APOPTOSIS
*CANCER cell proliferation
*OXIDATIVE stress
*ORGANOMETALLIC compounds
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Language
ISSN
0022-2623
Abstract
In this article, we report the findings of a comprehensivestructureâactivityrelationship study of N-(6-ferrocenyl-2-naphthoyl)dipeptide ethyl esters, in which novel analogues were designed, synthesized,and evaluated in vitrofor antiproliferative effect.Two new compounds, 2and 16, showed potentnanomolar activity in the H1299 NSCLC cell line, with exceptionalIC50values of 0.13 and 0.14 μM, respectively. Thesecompounds were also found to have significant activity in the Sk-Mel-28malignant melanoma cell line (IC50values of 1.10 and 1.06μM, respectively). Studies were also conducted to elucidatethe mode of action of these novel organometallic anticancer compounds.Cell cycle analysis in the H1299 cell line suggests these compoundsinduce apoptosis, while guanine oxidation studies confirm that 2is capable of generating oxidative damage via a ROS-mediatedmechanism. [ABSTRACT FROM AUTHOR]