ICG Montpellier-UMR 5253, Equipe AM2N, ENSCM, 8, Rue de l'Ecole Normale, 34296 Montpellier CEDEX 5, France; Université Mentouri-Constantine, Département de chimie, Laboratoire d'Obtention de Substances Thérapeutiques (LOST), Campus Chaabet Ersas, 25000 Constantine, Algeria.
Institut Européen des Membranes, cc047 Université de Montpellier 2, 34095 Montpellier, France.
Eur J Med Chem. 2015 Nov 2;104:33-41. doi: 10.1016/j.ejmech.2015.09.027. Epub 2015 Sep 28.
This paper describes the preparation and the biological evaluation of α-halogenated oxaphosphinanes. These halogen derivatives were synthetized from a short and stereoselective synthetic sequence starting by previously described hydroxy-precursors 1 and 2 with respectively a glucose and mannose-like configuration. The in vitro biological tests of these unnatural halogenated phosphinosugars, on several cell lines, highlighted, for some of them, their antiproliferative and anti migration and invasion properties at nanomolar concentration.
本文描述了α-卤代氧膦烷的制备和生物学评价。这些卤代衍生物是通过以前描述的具有葡萄糖和甘露糖样构型的羟基前体 1 和 2 ,经过简短的、立体选择性的合成序列合成的。这些非天然卤代膦糖在几种细胞系中的体外生物测试表明,其中一些在纳摩尔浓度下具有抗增殖、抗迁移和抗侵袭特性。