TY - CONF
T1 - Synthesis and antiproliferative activity of indazole derivatives
AU - Raffa, Demetrio
AU - Daidone, Giuseppe
AU - Maggio, Benedetta
AU - Cascioferro, Stella Maria
AU - Raimondi, Maria Valeria
AU - Plescia, Fabiana
PY - 2011
Y1 - 2011
N2 - 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
AB - 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
KW - CDK! inhibitors
KW - N-indazolylbenzamides
KW - antiproliferative activity.
KW - CDK! inhibitors
KW - N-indazolylbenzamides
KW - antiproliferative activity.
UR - http://hdl.handle.net/10447/55458
M3 - Other
SP - 76
EP - 76
ER -