- 期刊
Cytotoxic Evaluation of Bis-(α-Benzyl)Azatyrosylamides on Human Cancer Cell Lines
並列摘要
The antibiotic L-azatyrosine (1), an isostere of the coded L-tyrosine, was utilized as the lead compound for the development of potential anticancer agents. Previous studies have shown that a-benzylazatyrosines displayed an improved cytotoxic effect compared to the lead L-azatyrosine. These results have encouraged us in further investigations on the potential azatyrosine derivatives. Therefore, a series of alkyl-linked bis-(α-benzyl) azatyrosylamides 7a-f were synthesized. In vitro testing on human cancer cell line assay revealed that compounds with twoα-benzylazatyrosyl groups linked by short alkyl chains (e.g. 7b, c) exhibited 30- to 90-fold increases in cytotoxic potency against both OEC-Ml and BC-Ml cell lines as compared to L-azatyrosine and its monomeric constituent.
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