Synthesis and antiproliferative activity of indazole derivatives

Risultato della ricerca: Paper

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
Lingua originaleEnglish
Stato di pubblicazionePublished - 2011

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Indazoles
Derivatives
Hinges
Antineoplastic Agents
Hydrogen bonds

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title = "Synthesis and antiproliferative activity of indazole derivatives",
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",
keywords = "N-indazolylbenzamides, CDK! inhibitors, antiproliferative activity.",
author = "Giuseppe Daidone and Benedetta Maggio and Fabiana Plescia and Cascioferro, {Stella Maria} and Raimondi, {Maria Valeria}",
year = "2011",
language = "English",

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TY - CONF

T1 - Synthesis and antiproliferative activity of indazole derivatives

AU - Daidone, Giuseppe

AU - Maggio, Benedetta

AU - Plescia, Fabiana

AU - Cascioferro, Stella Maria

AU - Raimondi, Maria Valeria

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 - N-indazolylbenzamides, CDK! inhibitors, antiproliferative activity.

UR - http://hdl.handle.net/10447/55458

M3 - Paper

ER -