Abstract
Eighteen novel 3-substituted-indolin-2-ones containing chloropyrroles were synthesized and their biological activities were evaluated. The presence of a chlorine atom on the pyrrole ring was crucial to reduce cardiotoxicity. The presence of a 2-(ethyl-amino)ethylcarbamoyl group as a substituent at the C-4' position of the pyrrole enhanced the antitumor activities notably. IC50 values as low as 0.32, 0.67, 1.19 and 1.22 μM were achieved against non-small cell lung cancer (A549), oral epithelial (KB), melanoma (K111) and large cell lung cancer cell lines (NCI-H460), respectively.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / chemistry*
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Antineoplastic Agents / pharmacology
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Cell Line, Tumor / drug effects
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Chlorine / chemistry*
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Drug Screening Assays, Antitumor
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Humans
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Indoles / chemical synthesis*
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Indoles / chemistry*
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Intercellular Signaling Peptides and Proteins / metabolism
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Mice
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Molecular Structure
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Pyrroles / chemical synthesis*
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Pyrroles / chemistry*
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Vascular Endothelial Growth Factor Receptor-2 / antagonists & inhibitors
Substances
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Antineoplastic Agents
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Indoles
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Intercellular Signaling Peptides and Proteins
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Pyrroles
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indolin-2-one
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Chlorine
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Vascular Endothelial Growth Factor Receptor-2