Abstract
We have screened 11 isoquinoline derivatives and α-methylene-γ-butyrolactones using the 3-(4,5-dimethylthi-azol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) cytotoxicity assay in HeLa and HEK-293T cells. Compound 2 was identified as potential anticancer agent. To further improve its therapeutic potential, this agent was incorporated into transferrin (Tf)-conjugated liposomes (LPs) for targeted delivery to tumor cells. We have demonstrated Tf-LP-Compound 2 have superior antitumor activity compared to non-targeted controls and the free drug. These data show Tf-LP-Compound 2 to be a promising agent that warrants further evaluation.
MeSH terms
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Acrylates / administration & dosage*
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Acrylates / chemistry
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Antineoplastic Agents / administration & dosage*
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Antineoplastic Agents / chemistry
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Cell Line, Tumor
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Dose-Response Relationship, Drug
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Drug Carriers*
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Drug Screening Assays, Antitumor
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Endocytosis
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HEK293 Cells
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HeLa Cells
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Hep G2 Cells
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Humans
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Isoquinolines / administration & dosage*
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Isoquinolines / chemistry
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Lactones / chemistry
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Lactones / pharmacology
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Liposomes
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Membrane Potential, Mitochondrial / drug effects
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Quinolines / administration & dosage*
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Quinolines / chemistry
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Receptors, Transferrin / metabolism
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Transferrin / chemistry*
Substances
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Acrylates
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Antineoplastic Agents
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Drug Carriers
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Isoquinolines
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Lactones
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Liposomes
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Quinolines
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Receptors, Transferrin
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Transferrin
Grants and funding
The authors have no support or funding to report.