Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.name: Methyl 2-Boc-aminothiazole-4-carboxylate. In my other articles, you can also check out more blogs about 850429-62-8
850429-62-8, Name is Methyl 2-Boc-aminothiazole-4-carboxylate, molecular formula is C10H14N2O4S, belongs to thiazole compound, is a common compound. In a patnet, once mentioned the new application about 850429-62-8, name: Methyl 2-Boc-aminothiazole-4-carboxylate
Indoleamine 2,3-dioxygenase 1 (IDO1) and tryptophan 2,3-dioxygenase (TDO) are constitutively overexpressed in many types of cancer cells and exert important immunosuppressive functions. In this article, a series of 4,6-substituted-1H-indazole derivatives were synthesized and evaluated the inhibitory activities against IDO1 and TDO, as well as their structure-activity relationships (SARs). Among these, compound 35 displayed the most IDO1 inhibitory potency with an IC50 value of 0.74 muM in an enzymatic assay and 1.37 muM in HeLa cells. Quantitative analysis of the Western blot results indicated that 35 significantly decreased the INFgamma-induced IDO1 expression in a concentration-dependent manner. In addition, 35 showed promising TDO inhibition with an IC50 value of 2.93 muM in the enzymatic assay and 7.54 muM in A172 cells. Moreover, compound 35 exhibited in vivo antitumor activity in the CT26 xenograft model. These findings suggest that 1H-indazole derivative 35 is a potent IDO1/TDO dual inhibitor, and has the potential to be developed for IDO1/TDO-related cancer treatment.
Indoleamine 2,3-dioxygenase 1 (IDO1) and tryptophan 2,3-dioxygenase (TDO) are constitutively overexpressed in many types of cancer cells and exert important immunosuppressive functions. In this article, a series of 4,6-substituted-1H-indazole derivatives were synthesized and evaluated the inhibitory activities against IDO1 and TDO, as well as their structure-activity relationships (SARs). Among these, compound 35 displayed the most IDO1 inhibitory potency with an IC50 value of 0.74 muM in an enzymatic assay and 1.37 muM in HeLa cells. Quantitative analysis of the Western blot results indicated that 35 significantly decreased the INFgamma-induced IDO1 expression in a concentration-dependent manner. In addition, 35 showed promising TDO inhibition with an IC50 value of 2.93 muM in the enzymatic assay and 7.54 muM in A172 cells. Moreover, compound 35 exhibited in vivo antitumor activity in the CT26 xenograft model. These findings suggest that 1H-indazole derivative 35 is a potent IDO1/TDO dual inhibitor, and has the potential to be developed for IDO1/TDO-related cancer treatment.
Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.name: Methyl 2-Boc-aminothiazole-4-carboxylate. In my other articles, you can also check out more blogs about 850429-62-8
Reference£º
Thiazole | C3H8436NS – PubChem,
Thiazole | chemical compound | Britannica