Synthesis and biological evaluation of S-acyl-3-thiopropyl prodrugs of N-phosphonoacetyl-L-aspartate (PALA).

作者信息

Gagnard Valérie, Leydet Alain, Le Mellay Véronique, Aubenque Marielle, Morère Alain, Montero Jean-Louis

机构信息

Laboratoire de chimie biomoléculaire, UMR 5032, Université Montpellier II, ENSCM, 8 rue de l'Ecole normale, 34296 Montpellier cedex 5, France.

出版信息

Eur J Med Chem. 2003 Oct;38(10):883-91. doi: 10.1016/j.ejmech.2003.07.002.

DOI:10.1016/j.ejmech.2003.07.002

PMID:14575935

Abstract

The synthesis of new prodrugs of PALA characterised by the presence of S-acyl-3-thiopropyl, as enzyme-labile groups on the phosphonate moiety of PALA, is reported. The cytotoxic activities of PALA prodrugs were determined against human cell line (SW1573 lung carcinoma cells). A number of prodrugs bearing S-pivaloyl as acyl groups displayed cytotoxic activity in the same order of magnitude of PALA.

摘要