Suzuki–Miyaura cross-coupling, density functional theory, and auto-docking investigations were used to determine the effectiveness and stability of indazole derivatives.
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.
Synthesis of mono- and bis-thiosemicarbazones 4a–h and 5a–h of isatin–triazole hybrids 3a and 3b in turn accessed via CuAAC, their DFT studies and potential as phosphoinositide 3-kinase (PI3K) inhibitors has been evaluated in this study.
A general and authoritative literature overview on Pd-catalyzed cross-dehydrogenative coupling reactions of (hetero)arenes from the origins to 2023, where not only the synthetic aspects were described but also the most relevant mechanistic features.
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.