Nucleophilic opening of aryloxiranes with benzylpiperidine and subsequent rearrangement under Mitsunobu conditions led regioselectively to α-aryl-β-piperidinoalcohols and -amines. Amino-ifenprodil and indazole bioisosteres show high GluN2B affinity.
Fluorinated five-membered heterocycles have potent therapeutic activities including antiviral, anti-inflammatory, enzymatic inhibitory, and antimalarial.
Suzuki–Miyaura cross-coupling, density functional theory, and auto-docking investigations were used to determine the effectiveness and stability of indazole derivatives.
1H indazole derivatives with a ketoaryl groups at the 3-position were synthesized by a cyclisation reaction. All derivatives showed phosphorescence and/or double luminescence both in solution and the solid state.
This study focused on the development of a novel series of 5-ethylsulfonyl-indazole-3-carboxamides (8a–l) as dual inhibitors of VEGFR-2 and EGFR. Compounds 8g and 8h emerged as the most potent derivatives against breast (MCF-7) and colorectal (HCT-116) cancer cell lines.