Conformationally restrained analogues of ceramide containing thiouracil or uracil moieties in their polar head, substituted with an ethyl group in their 6-positions, proved to inhibit cell proliferation and induce apoptosis. A series of new thiouracil and uracil analogues of ceramide possessing several 6-alkyl- or 6-arylalkyl-substituents, were synthesized and tested as inhibitors of cell proliferation. The lipophilic substituents introduced in the 6-position were pure alkyls (n-propyl, n-butyl, i-butyl, neo-pentyl), or aryl-alkyls (2-phenylethyl). Although a significant antiproliferative activity was maintained in most compounds synthesized, none of them showed any improvement with respect to their 6-ethyl-substituted counterparts.
|Autori:||MACCHIA M; M. ANTONELLO; S. BERTINI; V. DI BUSSOLO; S. FOGLI; E. GIOVANNETTI; F. MINUTOLO; S. RAPPOSELLI; R. DANESI|
|Titolo:||Conformationally restrained ceramide analogues: effects of lipophilic modifications on the antiproliferative activity|
|Anno del prodotto:||2003|
|Digital Object Identifier (DOI):||10.1016/S0014-827X(02)00002-2|
|Appare nelle tipologie:||1.1 Articolo in rivista|