PROBLEM TO BE SOLVED: To obtain a novel vitamin D derivative that is useful as a therapeutic agent for hypercalcemia due to excessive vitamin D.MIURA DAISHIROU三浦 大志郎ISHIZUKA SEIICHI石塚 誠一OSONO KEIICHI大薗 恵一MANABE KENJI真鍋 健次...
PROBLEM TO BE SOLVED: To obtain a novel vitamin D3 derivative that is useful as a therapeutic agent for hypercalcemia due to excessive vitamin D. ;SOLUTION: This novel compound is a vitamin D3 derivative represented by formula I [m is 0-3; n is 0-2; X is O, S, NH; R1 and R2 ...
The Indole-Hydantoin Derivative Exhibits Anti-Inflammatory Activity by Preventing the Transactivation of NF-κB through the Inhibition of NF-κB P65 Phosphorylation at Ser276. Int. Immunopharmacol. 2021, 100, 108092. [Google Scholar] [CrossRef] Lee, T.H.; Khan, Z.; Kim, S.Y.; Lee, K.R...
Bisindigotin, a derivative of indigo and indirubin, demonstrated a dose-dependent (0.1–5 μM) inhibition of 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD)-induced ethoxyresorufin O-deethylase (EROD) activity in human HepG2 hepatoma cells with an IC50 of 0.8 μM [195]. In addition to its...
Another advantage of GATjm18 is its lipophilicity and molecular weight, which fit the Lipinski rules. When the thiazole was omitted, i.e., in GAT0913B, the activity was lost; but, if we incorporated a methyl group, at the furanyl moiety (derivative GAT0413), the activity was restored. ...
Applying Berthelot–Lorentz combining rules, the segment diameter σij and the dispersion-energy parameter uij in mixtures of substances i and j were estimated via Equations (6) and (7) [51]. An additional binary interaction parameter kij was required correcting the cross-dispersion energy between...
Ticlopidine Ticlopidine (5-[(2-chlorophenyl)methyl]-4,5,6,7-tetrahydrothieno[3,2-c]pyridine) is the first clinically useful thienopyridine derivative that inhibits platelet activation and aggregation by irreversibly blocking the ADP P2Y12 receptor [19]. Ticlopidine is a prodrug that in the body ...