Sun, Chiyu published the artcileSynthesis and Evaluation of Aminothiazole Derivatives as Hedgehog Pathway Inhibitors, HPLC of Formula: 22483-09-6, the main research area is aminothiazole Hedgehog inhibitor antitumor neoplasm; Gli1, hedgehog signaling; Smo; aminothiazole; benzimidazole; cytotoxicity; synthesis.
A series of aminothiazole derivatives bearing the benzimidazole moiety were synthesized and evaluated in Gli luciferase reporter assays. Lead optimization led to the discovery of potent hedgehog pathway antagonist (I) (2-[3-(1H-benzimidazol-2-yl)-4-chloroanilino]-N-[4-(trifluoromethyl)phenyl]-1,3-thiazole-4-carboxamide), with IC50 values in nanomolar range. The mol. basis ascribed to hindering sonic hedgehog-driven Smoothened (Smo) localization within the primary cilium (PC). Moreover, compound I inhibited Gli1 mRNA expression in mutant Smo cell line and displayed moderate cytotoxicity against DAOY cancer cell.
Chemistry & Biodiversity published new progress about Antitumor agents. 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, HPLC of Formula: 22483-09-6.
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