77779-60-3Relevant articles and documents
Synthesis and preliminary structure-activity relationship study of 2-aryl-2H-pyrazolo[4,3-c]quinolin-3-ones as potential checkpoint kinase 1 (Chk1) inhibitors
Malvacio, Ivana,Cuzzolin, Alberto,Sturlese, Mattia,Vera, D. Mariano A.,Moyano, E. Laura,Moro, Stefano
, p. 171 - 183 (2017/12/26)
The serine-threonine checkpoint kinase 1 (Chk1) plays a critical role in the cell cycle arrest in response to DNA damage. In the last decade, Chk1 inhibitors have emerged as a novel therapeutic strategy to potentiate the anti-tumour efficacy of cytotoxic chemotherapeutic agents. In the search for new Chk1 inhibitors, a congeneric series of 2-aryl-2 H-pyrazolo[4,3-c]quinolin-3-one (PQ) was evaluated by in-vitro and in-silico approaches for the first time. A total of 30 PQ structures were synthesised in good to excellent yields using conventional or microwave heating, highlighting that 14 of them are new chemical entities. Noteworthy, in this preliminary study two compounds 4e2 and 4h2 have shown a modest but significant reduction in the basal activity of the Chk1 kinase. Starting from these preliminary results, we have designed the second generation of analogous in this class and further studies are in progress in our laboratories.
New 1,8-naphthyridine and quinoline derivatives as CB2 selective agonists
Manera, Clementina,Cascio, Maria Grazia,Benetti, Veronica,Allara, Marco,Tuccinardi, Tiziano,Martinelli, Adriano,Saccomanni, Giuseppe,Vivoli, Elisa,Ghelardini, Carla,Di Marzo, Vincenzo,Ferrarini, Pier Luigi
, p. 6505 - 6510 (2008/09/20)
A series of new 1,8-naphthyridine and quinoline derivatives were synthesized and evaluated for their cannabinoid receptor affinity. In particular, compounds 2, 5, 11, and 13 showed a high CB2 affinity and CB2 versus CB1 selectivity, in agreement with molecular modeling studies. Furthermore, compound 2 also exhibited in vivo antinociceptive effects.
Structure-activity relationship studies at the benzodiazepine receptor (BZR): A comparison of the substituent effects of pyrazoloquinolinone analogs
Fryer,Zhang,Rios,Gu,Basile,Skolnick
, p. 1669 - 1673 (2007/10/02)
The synthesis of a series of 2-phenylpyrazolo[4,3-c]quinolin-3-one derivatives and their in vitro biological evaluation as ligands for the benzodiazepine receptor are described. The in vitro activities, as determined by an analysis of GABA shift ratios, a
