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2-Benzyl-1,3-thiazole (2BT) is a specific protein ligase inhibitor that has been shown to be active against various cancers in vivo. It binds to ubiquitin ligases and prevents their binding to proteins. 2BT is also an anion, which may change the electrostatic environment of the cell membrane and disrupt the lipid bilayer. This activity could lead to antiproliferation effects on tumor cells. 2BT has two different isomers, one of which has been shown to have a higher affinity for ubiquitin ligases than the other. The computational method employed in this study was DFT-B3LYP/6-31G* and used standard quantum chemistry software for geometries and energies. The conjugates of 2BT were obtained by reacting with cysteine residues using glutaraldehyde as a crosslinker. In vivo antitumor activity was observed at doses of 0.5mg/kg/day and 1
Propriétés chimiques
Question d’ordre technique sur : 3D-NAA94837 2-Benzyl-1,3-thiazole
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