Nonsteroidal Ligands for Estrogen Reception

摘要

Triphenyl-alkene derivatives of formula (I) are new. R1 = (CH2)nCR5=CR6R7; R2, R3 = H, Me, OH, OMe, OEt or i-Pr; R4 = CN, NO2, Me, Et, CH2CH2Y or Y; R5, R6 = H, 1-4C alkyl, 2-4C alkenyl, 2-4C alkynyl, X-(1-3C)alkyl, X-(2-4C)alkenyl, X-(2-4C)alkynyl or Y; R7 = CN, 1-4C hydroxyalkyl, CONR10R11, CONR12R13, CONHCH2R12, C(NH2)NOR12, SOR12, SO2OR12, SO2NHCO2R12, PO3R12, PO(NR12R13)(NR12R13), PO(NR12R13)(OR14), CONR12(CH2)qOMe, CONR12(CH2)qNR8R9 or oxadiazolyl substituted with Me; R8, R9 = H, 1-7C alkyl, 3-7C cycloalkyl, 1-7C alkoxy, (1-7C)alkyl-Y or phenyl; R10, R11 = Me or Et; or NR10R11 = morpholino; R12-R14 = H, 1-12C alkyl, 2-12C alkenyl, 2-12C alkynyl, 1-12C alkoxy, 2-12C alkenyloxy, 2-12C alkynyloxy, 3-7C cycloalkenyl, 3-7C cycloalkenyl (sic), linear and cyclic heteroalkyl, aryl, heteroaryl or Y; X = O or S; Y = halo; n = 0-2; and q = 1-12.