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Molecules ; 19(5): 6651-70, 2014 May 22.
Article in English | MEDLINE | ID: mdl-24858098

ABSTRACT

As part of a continuing search for new potential anticancer candidates, we describe the synthesis, cytotoxicity and mechanistic evaluation of a series of 4-oxoquinoline-3-carboxamide derivatives as novel anticancer agents. The inhibitory activity of compounds 10-18 was determined against three cancer cell lines using the MTT colorimetric assay. The screening revealed that derivatives 16b and 17b exhibited significant cytotoxic activity against the gastric cancer cell line but was not active against a normal cell line, in contrast to doxorubicin, a standard chemotherapeutic drug in clinical use. Interestingly, no hemolytical activity was observed when the toxicity of 16b and 17b was tested against blood cells. The in silico and in vitro mechanistic evaluation indicated the potential of 16b as a lead for the development of novel anticancer agents against gastric cancer cells.


Subject(s)
Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology , Animals , Antineoplastic Agents/chemical synthesis , Cell Line, Tumor/drug effects , Cell Membrane/drug effects , Chemistry Techniques, Synthetic , Computer Simulation , Doxorubicin/pharmacology , Drug Screening Assays, Antitumor , Erythrocytes/drug effects , Hemolytic Agents/pharmacology , Humans , Inhibitory Concentration 50 , Mice , Molecular Docking Simulation , Molecular Structure , Quinolones/chemistry , Stomach Neoplasms/drug therapy
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