Synthesis and preliminary biological assessments of a new class of amphiphilic telomers bearing 5-fluorouracil moieties

The synthesis and biological studies of cotelomers derived from tris(hydrox ymethyl)acrylamidomethane (THAM) and bearing 5-FU moieties are reported. Th ese macromolecular carriers were obtained by radical cotelomerization of TH AM and an N-1-acyloxymethyl derivative of 5-FU. Different telomers were pre pared in order to specify the influence of the prodrug on the efficiency of the therapeutic agent. An evaluation of their cytotoxic activity was perfo rmed in vitro on a melanoma cell line B16 using the colony-forming method. It appears from these biological assays that, while the monomeric substrate s are less active than free 5-FU, the multiplication of active ligands obta ined by telomerization involves a sharp enhancement of the antitumoral acti vity.