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Chromenopyrazole diones as cannabinoid quinone derivatives having anti-tumour activity

Authors: Jagerovic, Nadine; Morales, Paula; Goya, Pilar; Díaz-Laviada, Inés; Vara, Diana; Fernández-Ruiz, Javier; Gómez-Ruiz, M.; +1 Authors

Chromenopyrazole diones as cannabinoid quinone derivatives having anti-tumour activity

Abstract

[ES] La presente invención se refiere a un compuesto de fórmula general (I), O un tautómero, sal farmacéuticamente aceptable, profármaco osolvato del mismo, donde R1 se selecciona independientemente entre hidrógeno o alquilo C1-C18; R2 se selecciona independientemente entre hidrógeno, alquilo C1-C18 o arilo C5-C18; y R3 se selecciona independientemente entre hidrógeno o alquilo C1-C5. Además, la presente invención también hace referencia al uso del compuesto de fórmula (I) anterior para tratamiento de un cáncer o un tumor maligno, como por ejemplo blastoma, carcinoma, glioma, leucemia, linfoma y melanoma, asi como a un método para el tratamiento de dicho cáncer o tumor que comprende la administración de una cantidad terapéuticamente eficaz del compuesto de fórmula (I). Consecuentemente, una composición farmacéutica que comprende una cantidad terapéuticamente eficaz de un compuesto de fórmula general (I) y al menos un excipiente farmacéuticamente aceptable constituye otro de los aspectos de la invención. Es asimismo, objeto de la presente invención el procedimiento de obtención de dicho compuesto de fórmula general (I) mediante oxidación con [bis ( trifluoroacetoxi ) yodo ] benceno del correspondiente derivado fenólico precursor

[EN] The invention relates to a compound of general formula (I) or a tautomer, pharmaceutically acceptable salt, prodrug or solvate thereof, wherein R1 is independently selected from hydrogen or C1-C18 alkyl; R2 is independently selected from hydrogen, C1-C18 alkyl or C5-C18 aryl; and R3 is independently selected from hydrogen or C1-C5 alkyl. The invention also relates to the use of said compound of formula (I) for treating cancer or a malignant tumor, such as a blastoma, carcinoma, glioma, leukemia, lymphoma and melanoma, and to a method for treating said cancer or tumour, comprising the administration of a therapeutically effective quantity of the compound of formula (I). Consequently, the invention further relates to a pharmaceutical composition comprising a therapeutically effective quantity of a compound of general formula (I) and at least one pharmaceutically acceptable excipient. In addition, the invention relates to the method for producing said compound of general formula (I) by means of oxidation with [bis(trifluoroacetoxy)iode]benzene of the corresponding precursor phenolic derivative

Consejo Superior de Investigaciones Científicas, Universidad de Alcalá de Henares, Universidad Complutense de Madrid

A1 Solicitud de patente con informe sobre el estado de la técnica

Peer reviewed

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    influence
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    This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
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selected citations
These citations are derived from selected sources.
This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Citations provided by BIP!
popularity
This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
BIP!Popularity provided by BIP!
influence
This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Influence provided by BIP!
impulse
This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
BIP!Impulse provided by BIP!
0
Average
Average
Average
Green
Related to Research communities
Cancer Research