PROCEDES POUR L'IDENTIFICATION DE NOUVEAUX COMPOSES ACTIVATEURS DE ER ALPHA DANS LA PRODUCTION DU MONOXYDE D'AZOTE ENDOTHELIAL

摘要

In vitro method for screening and selecting chemical compounds derived from delphinidin activating the estrogen receptor (ER)alpha , comprises: obtaining at least one fused heterocylic compound (I); testing whether the compound activates the ERalpha ; and selecting the compound if it activates the estrogen receptor ERalpha . In vitro method for screening and selecting chemical compounds derived from delphinidin activating the estrogen receptor (ER)alpha , comprises: obtaining at least one fused heterocylic compound of formula (I); testing whether the compound activates the ERalpha ; and selecting the compound if it activates the estrogen receptor ERalpha . R 1-R 11 : H, halo (preferably F, Br or I), OH, amino, nitroso, nitro, CN, azonium, (1-6C)alkyl, (2-6C)alkenyl, (2-6C) alkynyl, (1-6C) haloalkyl, (1-6C) alkoxy, (1-6C) thioalkoxy, (1-6C) haloalkoxy, di ((1-6C) alkyl) amino or alkylcarbonyl; and X : a heteroatom comprising O, N or S (optionally charged and optionally substituted with a group of (1-6C) alkyl, (2-6C) alkenyl, (2-6C) alkynyl, (1-6C) haloalkyl, (1-6C) alkoxy, (1-6C) thioalkoxy, (1-6C) haloalkoxy, di ((1-6C) alkyl) amino, or alkylcarbonyl). An independent claim is included for in vitro method for screening and selecting chemical compounds derived from delphinidin activating the estrogen receptor (ER)alpha , comprises: obtaining at least one fused heterocylic compound (I); testing whether the compound activates the ERalpha ; and selecting the compound if it activates the estrogen receptor ERalpha . An independent claim is included for in vitro method for screening and selecting chemical compounds derived from delphinidin inducing the production of nitric oxide (NO) in endothelial cells, comprising: obtaining at least one compound (I); testing whether the compound induces the production of nitric oxide in endothelial cells with which it is contacted and selecting the compound if it induces the production of nitric oxide in endothelial cells with which it is contacted. [Image] ACTIVITY : Vasotropic; Cardiovascular-Gen.; Cytostatic; Cardiant; Antiarteriosclerotic; Hypotensive. MECHANISM OF ACTION : Estrogen receptor alpha activator; Nitric oxide production inducer.