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Synthesis and preliminary biological assessments of a new class of amphiphilic telomers bearing 5‐fluorouracil moieties
Author(s) -
Contino Christiane,
Maurizis Jean Claude,
Pucci Bernard
Publication year - 1999
Publication title -
macromolecular chemistry and physics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.57
H-Index - 112
eISSN - 1521-3935
pISSN - 1022-1352
DOI - 10.1002/(sici)1521-3935(19990601)200:6<1351::aid-macp1351>3.0.co;2-o
Subject(s) - telomerization , amphiphile , chemistry , prodrug , hydroxymethyl , biological activity , monomer , combinatorial chemistry , macromolecule , polymer chemistry , in vitro , organic chemistry , copolymer , biochemistry , polymer , catalysis
The synthesis and biological studies of cotelomers derived from tris(hydroxymethyl)acrylamidomethane (THAM) and bearing 5‐FU moieties are reported. These macromolecular carriers were obtained by radical cotelomerization of THAM and an N ‐1‐acyloxymethyl derivative of 5‐FU. Different telomers were prepared in order to specify the influence of the prodrug on the efficiency of the therapeutic agent. An evaluation of their cytotoxic activity was performed in vitro on a melanoma cell line B16 using the colony‐forming method. It appears from these biological assays that, while the monomeric substrates are less active than free 5‐FU, the multiplication of active ligands obtained by telomerization involves a sharp enhancement of the antitumoral activity.