Abstract
The synthesis of four benzophenone-containing analogues of the antiproliferative natural product didemnin B is presented. In vitro protein biosynthesis inhibition potency and antitumor activity were evaluated. The results indicate that all four analogues are biologically active and could serve as photoaffinity reagents for the study of receptor-binding interactions of didemnins. These analogues could also be useful in studying antitumor effects of didemnins.
Publication types
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Research Support, U.S. Gov't, Non-P.H.S.
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / pharmacology*
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Benzophenones / chemistry*
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Biological Factors / pharmacology
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Carrier Proteins / metabolism
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Cell Division / drug effects
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Depsipeptides*
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Humans
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Inhibitory Concentration 50
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Peptide Elongation Factor 1 / metabolism
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Peptides, Cyclic / chemical synthesis*
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Peptides, Cyclic / pharmacology*
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Photoaffinity Labels / metabolism
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Protein Biosynthesis / drug effects*
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Tumor Cells, Cultured
Substances
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Antineoplastic Agents
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Benzophenones
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Biological Factors
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Carrier Proteins
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Depsipeptides
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Peptide Elongation Factor 1
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Peptides, Cyclic
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Photoaffinity Labels
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didemnins
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benzophenone