Search results for "phosphonic acid analogues"
showing 2 items of 2 documents
Synthesis of phosphono dipeptides, inhibitors of cathepsin C
1998
Abstract Phosphono dipeptides containing glycine, glycylglycine or L-alanine at N-termini and racemic phosphonic acid analogues of aromatic amino acids, as well as racemic alicyclic aminophosphonates, exhibit moderate inhibitory activity towards cathepsin C. This activity is probably due to the binding of the phosphonate moiety by a positively charged part of the enzyme which is complementary to the carboxylate part of the synthetic dipeptide products of the enzymatic reaction.
Quinazoline antifolate thymidylate synthase inhibitors: replacement of glutamic acid by aminophosphonic acids
2003
The synthesis of six analogues of the potent thymidylate synthase (TS) inhibitor N -[4-[ N -[(3,4-dihydro-2-methyl-4-oxo-6-quinazolinoyl)-methyl]- N -prop-2-ynylamino]benzoyl]- L -glutamic acid 2 is described in which the glutamic acid residue has been replaced by DL -aminophosphonic acids. New antifolates were tested as inhibitors of TS isolated from mouse L1210 leukemic cells as well as inhibitors of growth mouse leukemic L5178Y cells. In general these modifications result in compounds that are considerably less potent than 2 as TS inhibitors with K i 's 0.17-1.10 w M. Very poor solubility in water limited their proper assay of growth cells inhibition.