CARBOXYLIC-ACID BIOISOSTERES OF GAMMA-LINKED DIPEPTIDE ANALOGS OF THEFOLATE-BASED THYMIDYLATE SYNTHASE (TS) INHIBITOR, -DESAMINO-2-METHYL-N-10-PROPARGYL-5,8-DIDEAZAFOLIC ACID (ICI-198583)

Authors
BAVETSIAS V JACKMAN AL KIMBELL R BOYLE FT BISSET GMF
Citation
V. Bavetsias et al., CARBOXYLIC-ACID BIOISOSTERES OF GAMMA-LINKED DIPEPTIDE ANALOGS OF THEFOLATE-BASED THYMIDYLATE SYNTHASE (TS) INHIBITOR, -DESAMINO-2-METHYL-N-10-PROPARGYL-5,8-DIDEAZAFOLIC ACID (ICI-198583), Bioorganic & medicinal chemistry letters, 6(6), 1996, pp. 631-636
Citations number
24
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
6
Year of publication
1996
Pages
631 - 636
Database
ISI
SICI code
0960-894X(1996)6:6<631:CBOGDA>2.0.ZU;2-2
Abstract
Tetrazole carboxylic acid bioisosteres of gamma-linked dipeptide deriv atives of -desamino-2-methyl-N-10-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 inhibi tory activities which, however, were not accompanied by a parallel imp rovement in the L1210 cell growth inhibition.