247174-85-2Relevant academic research and scientific papers
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.
Synthesis and antiproliferative activity of novel 3-(indazol-3-yl)- quinazolin-4(3H)-one and 3-(indazol-3-yl)-benzotriazin-4(3H)-one derivatives
Raffa, Demetrio,Daidone, Giuseppe,Maggio, Benedetta,Schillaci, Domenico,Plescia, Fabiana
, p. 317 - 320 (2007/10/03)
Several new 3-(indazol-3-yl)-quinazolin-4(3H)-one and 3-(indazol-3-yl)- benzotriazin-4(3H)-one derivatives 5 and 6 were synthesized and tested for their in vitro antiproliferative activity against Raji, K562, and K562-R cell lines. The pharmacological screening showed that some 2, 6, or 7-substituted quinazolinones 5 posses a significant antiproliferative activity, with a percentage growth inhibition ranging from 44.8% to 100% at 50 μM, which was higher than that showed by the unsubstituted derivative 5a previously synthesized. For the most active compounds 5d, 5f, and 5g the IC50 were recorded.
