1044255-57-3Relevant academic research and scientific papers
A novel thiazolidine compound induces caspase-9 dependent apoptosis in cancer cells
Onen-Bayram, F. Esra,Durmaz, Irem,Scherman, Daniel,Herscovici, Jean,Cetin-Atalay, Rengul
, p. 5094 - 5102 (2012)
The forward chemogenomics strategy allowed us to identify a potent cytotoxic thiazolidine compound as an apoptosis-inducing agent. Chemical structures were designed around a thiazolidine ring, a structure already noted for its anticancer properties. Initially, we evaluated these novel compounds on liver, breast, colon and endometrial cancer cell lines. The compound 3 (ALC67) showed the strongest cytotoxic activity (IC50 ～5 μM). Cell cycle analysis with ALC67 on liver cells revealed SubG1/G1 arrest bearing apoptosis. Furthermore we demonstrated that cytotoxicity of this compound was due to the activation of caspase-9 involved apoptotic pathway, which is death receptor independent.
Design, synthesis and evaluation of potent thymidylate synthase X inhibitors
Esra Oenen,Boum, Yap,Jacquement, Claire,Spanedda, Maria Vittoria,Jaber, Nada,Scherman, Daniel,Myllykallio, Hannu,Herscovici, Jean
scheme or table, p. 3628 - 3631 (2009/04/06)
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.
