Design, synthesis and evaluation of potent thymidylate synthase X inhibitors.
Three synthesized series of compounds based on a thiazolidine core allowed identification of potent inhibitors of thymidylate synthase X. The evaluation of the catalytic activity of the enzyme in the presence of these molecules revealed two distinct classes of compounds that inhibit ThyX with submicromolar concentrations, which could lead, after optimization, to effective inhibitors with potential biomedical interest.
Unité de Pharmacologie Chimique et Génétique, Ecole Nationale Supérieure de Chimie de Paris, Paris, France.
F
F
Esra Onen
Yap
Y
Boum
Claire
C
Jacquement
Maria Vittoria
MV
Spanedda
Nada
N
Jaber
Daniel
D
Scherman
Hannu
H
Myllykallio
Jean
J
Herscovici
D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D008968:Molecular Conformation; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D053778:Thiazolidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013940:Thymidylate Synthase / Q000037:antagonists & inhibitors* / Q000737:chemistry; D013997:Time Factors
D004791:Enzyme Inhibitors; D053778:Thiazolidines; D013940:Thymidylate Synthase