Add time:08/01/2019 Source:sciencedirect.com
Tetrazole carboxylic acid bioisosteres of γ-linked dipeptide derivatives of 2-desamino-2-methyl-N10-propargyl-5,8-dideazafolic acid (ICI 198583), a folate-based inhibitor of thymidylate synthase (TS), were synthesised by multistep routes starting from the appropriate pteroic acid analogue and Z-d-Ala or d-Glu. They exhibited excellent TS inhibitory activities which, however, were not accompanied by a parallel improvement in the L1210 cell growth inhibition.
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