Abstract
In order to obtain new compounds with antitumoural action the N-(meta-acylaminobenzoyl)-alpha-acylaminobenzoyl)-alpha-aminoacids 4-9 were prepared. These compounds were subsequently converted into the corresponding Delta(2)-oxazolin-5-ones 10-15, which in turn were submitted to a ring opening reaction with di-(beta-chloroethyl)amine to afford the peptide supported N-mustards 16-21, which showed low toxicity and cytostatic activity similar to that of sarcolisine against the Ehrlich ascite and Walker 253 carcinosarcoma.
MeSH terms
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Alkylation / drug effects
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Amides / chemical synthesis*
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Amides / chemistry
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Amides / pharmacology
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Amino Acids / chemical synthesis*
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Amino Acids / chemistry
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Amino Acids / pharmacology
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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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Benzoates / chemical synthesis*
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Benzoates / chemistry
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Benzoates / pharmacology
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Cell Line, Tumor
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Drug Screening Assays, Antitumor
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Magnetic Resonance Spectroscopy
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Mice
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Protons
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Rats
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Rats, Wistar
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Spectrophotometry, Infrared
Substances
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Amides
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Amino Acids
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Antineoplastic Agents
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Benzoates
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Protons