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GIUSEPPE DAIDONE

N-(INDAZOLYL)BENZAMIDO DERIVATIVES AS CDK1 INHIBITORS: DESIGN, SYNTHESIS, BIOLOGICAL ACTIVITY, AND MOLECULAR DOCKING STUDIES

  • Autori: Raffa, D.; Maggio, B.; Cascioferro, S.; Raimondi, M.; Daidone, G.; Plescia, S.; Schillaci, D.; Cusimano, M.; TITONE LANZA DI SCALEA, L.; Colomba, C.; Tolomeo, M.
  • Anno di pubblicazione: 2009
  • Tipologia: Articolo in rivista (Articolo in rivista)
  • Parole Chiave: N-(1H-indazolyl)benzamides, 1H-indazole-3-carboxamides, CDK1, Molecular docking

Abstract

A series of N-1H-indazole-1-carboxamides have been synthesized and their effects on both CDK1/cyclin B and K-562 (human chronic myelogenus leukemia) cell line were evaluated. Using a computational model we have observed that all the most active compound 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 resulted non cytotoxic against HuDe (IZSL), primary cell cultures from human derm. These preliminary results are quite encouraging in view of the low toxicity showed by the above mentioned compounds.

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