| Assay Method Information | |
| | VEGFR tyrosine kinase inhibition |
| Description: | In a representative synthetic procedure (compound 3), a mixture of 1 (330 mg, 2 mM) and 3-F3C-C6H4-NHNH2 (370 mg, 2.1 mM) in anisole (20 mL) was stirred at reflux for 10 h. The resulting dark yellow mixture was cooled down, diluted with 50 mL of EtOAc and washed with 2 · 25 mL of saturated aqueous NaHCO3. Organic phase was dried over anhydrous Na2SO4 and concentrated. Solid residue was triturated with 3 · 10 mL of a 3:1 mixture (v/v) of Et2O and EtOAc to give triazole 2 (352 mg, 58% yield). Intermediate 2 (304 mg, 1 mM) was treated with 4-Py-COCl (170 mg, 1.2 mM) in 10 mL of pyridine at room temperature. The resulting dark yellow solution was stirred at room temperature for 12 h, poured into 25 mL of saturated NaHCO3, extracted with 3 · 20 mL of EtOAc. The combined organic extract was washed with 3 · 10 mL of water, dried over anhydrous Na2SO4 and concentrated. Solid residue was triturated with 3 · 10 mL of Et2O. Toluene (50 mL) followed by P4S10 (2.22 g, 5 mM) was added to the r |
| Affinity data for this assay | |
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