| 摘要 |
Angiogenesis, tumor growth, and metalloproteinase 2(MMP2) interaction with integrin-.alpha.v.beta.3 are inhibited by an inhibitor compound of formula (I): wherein G1 and G2 are each independently NH- C(O)-O-R1, -NH-C(O)-O-(CH2)v-(C6H4)-X3, -NH-C(O)-NH-(CH2)v-(C6H4)-X3, -O-C(O)-NH-(CH2)v-(C6H4)-X3,-O-C(O)-O-(CH2)v- (C6H4)-X3, or NH-C(O)-CH2-(C6H4)-X3; Y1 and Y2 are each independently OH, C1-C4 alkyl, C1-C4 hydroxyalkyl, C1-C4 alkoxy, phenyl, benzyl, or NH2; R1 is C1-C4 alkyl; X1 and X2 are each independently halo or C1-C4 alkoxy; X3 is halo, nitro, C1-C4 alkyl, C1-C4 alkoxy, or C1-C4 perfluoroalkyl; Z is -C.ident.C-, -C6H4-, cis-CH=CH-, trans CH=CH-, cis-CH2-CH=CH-CH2-, trans -CH2-CH=CH-CH2-, 1,4-naphthyl, cis-1,3-cyclohexyl, trans-1, 3-cyclohexyl, cis-1, 4-cyclohexyl, or trans-1,4-cyclohexyl; A is H or a covalent bond; m and n are each independently an integer having a value of 0 or 1; t is an integer having a value of 0 or 1; and p, r , and v are each independently an integer having a value of 1 or 2; with provisos that when A is H, t is O; when A is a covalent bond, t is 1; when m is 0, Y1 is C1-C4 hydroxyalkyl; and when n is 0, Y2 is C1 C4 hydroxyalkyl.
|
