Angiogenesis, tumor growth, and metalloproteinase 2 (MMP2) interaction
with integrin-.alpha..sub.v.beta..sub.3 are inhibited by an inhibitor
compound of formula (I): wherein G.sup.1 and G.sup.2 are each
independently NH--C(O)--O--R.sup.1,
--NH--C(O)--O--(CH.sub.2).sub.v--(C.sub.6H.sub.4)--X.sup.3,
--NH--C(O)--NH--(CH.sub.2).sub.v--(C.sub.6H.sub.4)--X.sup.3,
--O--C(O)--NH--(CH.sub.2).sub.v--(C.sub.6H.sub.4)--X.sup.3,
--O--C(O)--O--(CH.sub.2).sub.v--(C.sub.6H.sub.4)--X.sup.3, or
NH--C(O)--CH.sub.2--(C.sub.6H.sub.4)--X.sup.3; Y.sup.1 and Y.sup.2 are
each independently OH, C.sub.1 C.sub.4 alkyl, C.sub.1 C.sub.4
hydroxyalkyl, C.sub.1 C.sub.4 alkoxy, phenyl, benzyl, or NH.sub.2;
R.sup.1 is C.sub.1 C.sub.4 alkyl; X.sup.1 and X.sup.2 are each
independently halo or C.sub.1 C.sub.4 alkoxy; X.sup.3 is halo, nitro,
C.sub.1 C.sub.4 alkyl, C.sub.1 C.sub.4 alkoxy, or C.sub.1 C.sub.4
perfluoroalkyl; Z is --C.ident.C--, --C.sub.6H.sub.4--, cis-CH.dbd.CH--,
trans CH.dbd.CH--, cis-CH.sub.2--CH.dbd.CH--CH.sub.2--, trans
--CH.sub.2--CH.dbd.CH--CH.sub.2--, 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, Y.sup.1 is C.sub.1 C.sub.4 hydroxyalkyl; and when n is 0,
Y.sup.2 is C.sub.1 C.sub.4 hydroxyalkyl.
