78155-75-6Relevant articles and documents
Synthesis and anticancer evaluation of indazole-aryl hydrazide-hydrazone derivatives
Rudavath, Durgesh,Sreenivasulu, Reddymasu,Pinapati, Srinivasa Rao,Raju, Rudraraju Ramesh
, p. 433 - 438 (2020/06/29)
A new series of hydrazide-hydrazones linked between indazole and substituted benzaldehydes were designed, synthesized and evaluated for their cytotoxicity against four human cancer cell lines (HeLa, MDA-MB-231, MCF-7 and A549). Among the synthesized compo
Optimization of N-benzoylindazole derivatives as inhibitors of human neutrophil elastase
Crocetti, Letizia,Schepetkin, Igor A.,Cilibrizzi, Agostino,Graziano, Alessia,Vergelli, Claudia,Giomi, Donatella,Khlebnikov, Andrei I.,Quinn, Mark T.,Giovannoni, Maria Paola
, p. 6259 - 6272 (2013/09/02)
Human neutrophil elastase (HNE) is an important therapeutic target for treatment of pulmonary diseases. Previously, we identified novel N-benzoylindazole derivatives as potent, competitive, and pseudoirreversible HNE inhibitors. Here, we report further development of these inhibitors with improved potency, protease selectivity, and stability compared to our previous leads. Introduction of a variety of substituents at position 5 of the indazole resulted in the potent inhibitor 20f (IC50 ～10 nM) and modifications at position 3 resulted the most potent compound in this series, the 3-CN derivative 5b (IC50 = 7 nM); both derivatives demonstrated good stability and specificity for HNE versus other serine proteases. Molecular docking of selected N-benzoylindazoles into the HNE binding domain suggested that inhibitory activity depended on geometry of the ligand-enzyme complexes. Indeed, the ability of a ligand to form a Michaelis complex and favorable conditions for proton transfer between Hys57, Asp102, and Ser195 both affected activity.
POLYCYCLIC INDAZOLE DERIVATIVES AND THEIR USE AS ERK INHIBITORS FOR THE TREATMENT OF CANCER
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Page/Page column 272, (2009/01/24)
Disclosed are the ERK inhibitors of formula 1.0: (Chemical formula should be inserted here as it appears on abstract in paper form) and the pharmaceutically acceptable salts, esters and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.
