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GIUSEPPE DAIDONE

Synthesis and antiproliferative activity of indazole derivatives

  • Autori: Raffa, D.; Maggio, B.; Raimondi, M.; Cascioferro, S.; Plescia, F.; Tolomeo, M.; Daidone, G.
  • Anno di pubblicazione: 2011
  • Tipologia: Proceedings (TIPOLOGIA NON ATTIVA)
  • Parole Chiave: N-indazolylbenzamides, CDK! inhibitors, antiproliferative activity.

Abstract

Indazole nucleus represents a very attractive scaffol to obtain new molecole endowed with antineoplastic activity. On the basis of these literature data we have designed some indazole derivatives such as N-indazolylbenzamides and N-indazolyl-N’-phenylureas as potential CDK1 inhibitors. In fact the above compounds contain the structural feature, common to the majority of CDK inhibitors, requested to make hydrogen bonds with the molecular forks present in the hinge region of CDKs. The N-indazolylbenzamides 1 were obtained by reacting aminoindazoles and substituted benzoylchlorides. Among the synthesized compounds some derivatives 1 resulted to be CDK1 inhibitors showing IC50 values in the range 4.4-10.0 M