A set of variously substituted 1-arylpyrazol-3-one derivatives, including the di-ortho-aryl substituted ones, was synthesized as new potential anticancer compounds. To fulfill this aim, herein a regiospecific synthesis was proposed utilizing a new revisited one pot procedure, starting from commercial anilines and easily accessible 2,5-dimethyl-furan-3-one. In the course of the sequential ordered steps, in some cases, a nitro group displacement by chlorine took place to a minor extent. The in vitro screening against the full panel of ~60 human cancer cell lines (NCI) showed a moderate, but promising selective antiproliferative activity against the UO31 renal tumor cell line, only in compounds with the introduction on the phenyl moiety of a -CF3 or two Cl groups.

Mingoia F., Panzeca G., Vitale M.C., La Monica G., Bono A., Lauria A., et al. (2022). One pot-like regiospecific access to 1-aryl-1H-pyrazol-3(2H)-one derivatives and evaluation of the anticancer activity. ARKIVOC, 2022(2), 191-203 [10.24820/ark.5550190.p011.739].

One pot-like regiospecific access to 1-aryl-1H-pyrazol-3(2H)-one derivatives and evaluation of the anticancer activity

Panzeca G.;La Monica G.;Bono A.;Lauria A.;Martorana A.
Ultimo
2022-04-04

Abstract

A set of variously substituted 1-arylpyrazol-3-one derivatives, including the di-ortho-aryl substituted ones, was synthesized as new potential anticancer compounds. To fulfill this aim, herein a regiospecific synthesis was proposed utilizing a new revisited one pot procedure, starting from commercial anilines and easily accessible 2,5-dimethyl-furan-3-one. In the course of the sequential ordered steps, in some cases, a nitro group displacement by chlorine took place to a minor extent. The in vitro screening against the full panel of ~60 human cancer cell lines (NCI) showed a moderate, but promising selective antiproliferative activity against the UO31 renal tumor cell line, only in compounds with the introduction on the phenyl moiety of a -CF3 or two Cl groups.
Settore CHIM/08 - Chimica Farmaceutica
https://www.arkat-usa.org/arkivoc-journal/browse-arkivoc/ark.5550190.p011.739
Mingoia F., Panzeca G., Vitale M.C., La Monica G., Bono A., Lauria A., et al. (2022). One pot-like regiospecific access to 1-aryl-1H-pyrazol-3(2H)-one derivatives and evaluation of the anticancer activity. ARKIVOC, 2022(2), 191-203 [10.24820/ark.5550190.p011.739].
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/10447/576095
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