Derivatives of naftofuran and naftotiofeno as antiproliferative agents of the cancer of pancreas and colon. (Machine-translation by Google Translate, not legally binding)

Derivatives of benzo [b] naphtho [1,2-d] furan, benzo [b] naphtho [1,2-d] thiophene, 2-arylnaphtho [2,1-b] furan and 2-arylnaphtho [2,1- b] thiophene of general formulas i and ii, where r1, r2, y and z can be different types of atoms, chains and groups usually used in organic chemistry, characterize...

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Hauptverfasser: RAMOS GONZALEZ ANA MARIA, HIDALGO MEDINA MANUEL, RODRIGUEZ MARTIN JOSE JUAN, LOPEZ CASAS PEDRO P, MARTIN SANTAMARIA SONSOLES, DE PASCUAL-TERESA FERNANDEZ BEATRIZ
Format: Patent
Sprache:eng ; spa
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Zusammenfassung:Derivatives of benzo [b] naphtho [1,2-d] furan, benzo [b] naphtho [1,2-d] thiophene, 2-arylnaphtho [2,1-b] furan and 2-arylnaphtho [2,1- b] thiophene of general formulas i and ii, where r1, r2, y and z can be different types of atoms, chains and groups usually used in organic chemistry, characterized by their potential antiproliferative capacity; in particular, 3,9-dihydroxybenzo [b] naphtho [1,2-d] furan-5-carbonitrile and 3,9-dihydroxybenzo [b] naphtho [1,2-d] thiophene-5-carbonitrile inhibit the proliferation of human malignant cells of pancreas and colon in values higher than the inhibition caused by gemcitabine and 5-fluorouracil, compounds that are used in the treatment of these two types of tumors respectively. Systems i and ii are synthesized by condensation between a compound with active hydrogens and the corresponding aldehyde in basic medium, followed by a photochemical electrocylic closure under oxidizing conditions to promote the aromatization of the formed product, obtaining the different compounds or possible reduction derivatives or hydrolysis, prodrugs and medications for use in anticancer therapy, by any means available in the clinic. (Machine-translation by Google Translate, not legally binding) Derivados de benzo[b]nafto[1,2-d]furano, benzo[b]nafto[1,2-d]tiofeno, 2-arilnafto[2,1-b]furano y 2-arilnafto[2,1-b]tiofeno de fórmulas generales I y II, donde R1, R2, Y y Z pueden ser diferentes tipos de átomos, cadenas y grupos habitualmente utilizados en química orgánica, caracterizados por su potencial capacidad antiproliferativa; en particular, 3,9-dihidroxibenzo[b]nafto[1,2-d]furano-5-carbonitrilo y 3,9-dihidroxibenzo[b]nafto[1,2-d]tiofeno-5-carbonitrilo inhiben la proliferación de células humanas malignas de páncreas y colon en unos valores superiores a la inhibición provocada por la gemcitabina y el 5-fluorouracilo, compuestos que se utilizan en el tratamiento de estos dos tipos de tumores respectivamente. Los sistemas I y II son sintetizados por condensación entre un compuesto con hidrógenos activos y el correspondiente aldehído en medio básico, seguido de un cierre electrocíclico fotoquímico en condiciones oxidantes para promover la aromatización del producto formado, obteniéndose los diferentes compuestos o posibles derivados de reducción o hidrólisis, profármacos y medicamentos para su utilización en la terapia anticancerosa, por cualquier medio disponible en clínica.