RESUMEN
In this study, the synthetic way to new N-pyridinyl(methyl)indolylpropanamides acting as non acidic NSAIDs has been described. Pharmacomodulation was carried out at N(1) and C(5) of the indole ring and at the level of the propanamide chain. N(3)-pyridinylmethyl-[1(4-chlorobenzyl-5-chloroindol-3-yl)propanamide represents one of the most potent compounds in the TPA-induced mouse ear swelling assay, with a level of activity higher than that of ibuprofen and comparable to that of dexamethasone.
Asunto(s)
Amidas/síntesis química , Indoles/síntesis química , Inflamación/tratamiento farmacológico , Amidas/farmacología , Animales , Dexametasona , Ibuprofeno , Indoles/farmacología , Inflamación/prevención & control , Ratones , Relación Estructura-ActividadRESUMEN
Several N-pyridinyl(methyl)-indol-3-ylpropanamides were synthesized and pharmacological evaluations of their immunosuppressive potential were performed. Among thirteen compounds tested in vitro on murine T proliferation, three showed interesting inhibiting activity. For the most active compound (propanamide 18), immunosuppressive activity was documented both in vitro on human T lymphocytes proliferation and in vivo on mice delayed-type hypersensitivity. These experimental data demonstrated that these compounds hold potential as immunosuppressive agents.
Asunto(s)
Inmunosupresores/farmacología , Indoles/farmacología , Piridinas/farmacología , Amidas/química , Animales , Proliferación Celular , Femenino , Humanos , Hipersensibilidad Tardía , Indoles/química , Ratones , Ratones Endogámicos BALB C , Piridinas/química , Linfocitos T/efectos de los fármacosRESUMEN
New series of 2(or 3)-arylmethylenenaphtho[2,1-b]furan-3(or 2)-ones were synthesized, characterized and tested for anticancer properties in vitro. The target compounds were prepared by Knoevenagel coupling between the naphthofuranones 3, 28-30 and formyl derivatives. 2-(4-Oxo-1-benzopyran-3-ylmethylene)naphtho[2,1-b]furan-3-one 36 was the most active compound (IC50 (L1210) = 1.6 microM). These compounds were also evaluated, in an independent manner, as inhibitors of Src protein tyrosine kinase, but only minor activity was observed.