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Experimental Chemotherapy

Antitumor Activity of a New N-Substituted Thiourea Derivative, an EGFR Signaling-Targeted Inhibitor against a Panel of Human Lung Cancer Cell Lines

Xiong X.a · Liu H.b · Fu L.a · Li L.a · Li J.b · Luo X.b · Mei C.a

Author affiliations

aNephrology Institute of PLA, Department of Internal Medicine, Changzheng Hospital, Second Military Medical University, and bDrug Discovery and Design Centre, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Graduate School of the Chinese Academy of Sciences, Chinese Academy of Sciences, Shanghai, PR China

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Chemotherapy 2008;54:463–474

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Article / Publication Details

First-Page Preview
Abstract of Experimental Chemotherapy

Received: January 28, 2008
Accepted: June 27, 2008
Published online: October 02, 2008
Issue release date: October 2008

Number of Print Pages: 12
Number of Figures: 7
Number of Tables: 2

ISSN: 0009-3157 (Print)
eISSN: 1421-9794 (Online)

For additional information: http://www.karger.com/CHE

Abstract

Epidermal growth factor receptor (EGFR) is one of the important protein tyrosine kinases (PTKs), whose blockade by tyrosine kinase inhibitors (TKIs) has been introduced in the treatment of advanced non-small-cell lung cancers (NSCLCs). However, intrinsic and acquired resistance to the clinically used erlotinib or gefitinib leads to poor overall prognosis. The novel EGFR-TKI will provide alternative choices in NSCLC treatment and might be beneficial. We have previously reported the design and synthesis of a novel class of PTK inhibitors featuring the N-(2-oxo-1,2-dihydro-quinolin-3-ylmethyl)-thiourea framework. In this study, we examined the antitumor effect of compound 5a (DC27) in a panel of human lung carcinoma cell lines. The results of a bromodeoxyurdine (BrdU) incorporation assay revealed that cell proliferation was inhibited in a dose-dependent manner, with an IC50 of 2.5–12.9 µM, similar to gefitinib (1.1–15.6 µM). DC27 induced G₀/G1 arrest of cell cycle and apoptosis as tested by flow cytometry. DC27 markedly reduced tyrosine phosphorylation of EGFR and inhibited activation of Erk1/2 and AKT, two key downstream effectors of proliferation. In conclusion, DC27 has potent in vitro cytotoxicity against human lung carcinoma cells, possibly mediated by induction of apoptosis and cell cycle arrest in G₀/G1 phase.

© 2008 S. Karger AG, Basel


Article / Publication Details

First-Page Preview
Abstract of Experimental Chemotherapy

Received: January 28, 2008
Accepted: June 27, 2008
Published online: October 02, 2008
Issue release date: October 2008

Number of Print Pages: 12
Number of Figures: 7
Number of Tables: 2

ISSN: 0009-3157 (Print)
eISSN: 1421-9794 (Online)

For additional information: http://www.karger.com/CHE


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Drug Dosage: The authors and the publisher have exerted every effort to ensure that drug selection and dosage set forth in this text are in accord with current recommendations and practice at the time of publication. However, in view of ongoing research, changes in government regulations, and the constant flow of information relating to drug therapy and drug reactions, the reader is urged to check the package insert for each drug for any changes in indications and dosage and for added warnings and precautions. This is particularly important when the recommended agent is a new and/or infrequently employed drug.
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