The Effect of a Newly Synthesized Indazole Compound, TAS-3-124, on Experimental Autoimmune Disease

3-O-Formyl-20R,21-epoxyresibufogenin suppresses IL-6–type cytokine actions by targeting the glycoprotein 130 subunit: Potential clinical implications

“…IL-6 stimulates transcription of the AACT gene by activating STAT3, which binds to the STAT3-responsive element located -95 to -87 base pairs upstream of the transcription-initiation site of the AACT gene. 17 TAS-3-124 was used as a control for these compounds because TAS-3-124 is an active chemical, suppressing inflammation by inhibiting IL-6 production in mice, 18 rather than using biologically inactive bufogenins. TB-2-081 and TB-2-082 dose-dependently suppressed IL-6-induced expression of the AACT mRNA in HepG2 cells (respectively by as much as 56% and 41% at 10 mmol/L of concentration, P < .01, compared with results obtained in the absence of TB-2-081), whereas the control TAS-3-124 failed to do so (Fig 1, A).…”

Recent Advances in the Chemistry of Indazoles

“…The latter mentioned compounds are examples for C(6)‐monosubstituted indazoles of pharmacolocical interest, only few examples of this group are described 45. Two additional examples are TAS‐3–12446 and 29 42. Biologically interesting indazoles substituted at C(7) are represented by 30 and 31 .…”

“…The latter mentioned (7‐NI 31 ) and related indazoles were also shown to exhibit antinociceptive and cardiovascular effects 51. Several substituted indazoles and potential analogues of 7‐NI have been reported45,46 from which 7‐methoxyindazole proved to be the most active compound in in vitro enzymatic assays of nNOS activity 52 . N ‐(7‐Indazolyl)benzenesulfonamide derivatives were prepared and investigated as cell cycle inhibitors 53…”