883054-87-3Relevant articles and documents
N-(indazolyl)benzamido derivatives as CDK1 inhibitors: Design, synthesis, biological activity, and molecular docking studies
Raffa, Demetrio,Maggio, Benedetta,Cascioferro, Stella,Raimondi, Maria Valeria,Daidone, Giuseppe,Plescia, Salvatore,Schillaci, Domenico,Cusimano, Maria Grazia,Titone, Lucina,Colomba, Claudia,Tolomeo, Manlio
experimental part, p. 265 - 273 (2009/09/06)
A series of N-1H-indazole-1-carboxamides has been synthesized and their effects on both CDK1 / cyclin B and the K-562 (human chronic myelogenus leukemia) cell line were evaluated. Using a computational model, we have observed that all the most active compounds 9e, f, i-n exhibited the same binding mode of purvanalol A in the ATP-binding cleft. Although they were able to moderately inhibit the leukemic cell line K-562 and to show inhibitory activity against the Cdc2-Cyclin B kinase in the low micromolar range, they turned out to be non-cytotoxic against HuDe (IZSL) primary cell cultures from human derm. These preliminary results are quite encouraging in view of the low toxicity demonstrated by the above-mentioned compounds.
