Methods for inhibiting angiogenesis and tumor growth
AssigneeThe Scripps Research Institute
InventorsDale L. Boger, David A. Cheresh
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AssigneeThe Scripps Research Institute
InventorsDale L. Boger, David A. Cheresh
Estimating the term…
Angiogenesis, tumor growth, and metalloproteinase 2 (MMP2) interaction with integrin-αvβ3 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≡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.
A method of inhibiting the interaction of MMP2 with integrin αvβ3 in a host cell which comprises contacting the integrin with an interaction inhibiting amount of a compound represented by the formula:
A method of inhibiting the interaction of MMP2 with integrin αvβ3 in a host cell which comprises contacting the integrin with an interaction inhibiting amount of a compound represented by the formula:
Dependencies are inferred from the claim text.