Abstract
Six selected diketopiperazines, cyclo(Gly-Val), cyclo(Gly-D-Val), cyclo(Gly-Leu), cyclo(Gly-Ile), cyclo(Phe-Cys) and cyclo(Tyr-Cys), were synthesized via various synthetic routes. Their potential to inhibit cancer cell growth in HT-29, HeLa and MCF-7 cells was determined. Cyclo(Tyr-Cys) caused the greatest inhibition in cervical carcinoma cells with near equivalent activity against HT-29 and MCF-7 cells. The other cyclic dipeptides tested were effective in the inhibition of colon, cervical and breast carcinoma cells, respectively, but the percentage inhibition was lower than for cyclo(Tyr-Cys).
MeSH terms
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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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Carcinoma / drug therapy*
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Cell Line, Tumor
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Chromatography, High Pressure Liquid
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Diketopiperazines / chemical synthesis*
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Diketopiperazines / chemistry
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Diketopiperazines / pharmacology
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Drug Screening Assays, Antitumor
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Female
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HT29 Cells
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HeLa Cells
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Humans
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Mass Spectrometry
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Microscopy, Electron, Scanning
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Molecular Structure
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Neoplasms / drug therapy*
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Peptides, Cyclic / chemical synthesis*
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Peptides, Cyclic / chemistry
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Peptides, Cyclic / pharmacology
Substances
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Antineoplastic Agents
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Diketopiperazines
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Peptides, Cyclic