Abstract
We prepared an analogue of an antitumor bicyclic hexapeptide RA-VII whose amide configuration between residues 2 and 3 was fixed to cis by incorporating a triazole cis-amide bond surrogate. This analogue was shown, by NMR studies, to take almost the same conformation as that of the minor conformer of RA-VII. It showed no cytotoxic activity.
MeSH terms
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Alanine / chemistry
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Amides / chemistry
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / toxicity
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Peptides, Cyclic / chemical synthesis
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Peptides, Cyclic / chemistry
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Peptides, Cyclic / toxicity
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Triazoles / chemistry*
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Tyrosine / chemistry
Substances
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Amides
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Antineoplastic Agents
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Peptides, Cyclic
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Triazoles
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Tyrosine
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RA VII
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Alanine