METHOD FOR INHIBITION OF ANGIOGENESIS AND TUMOR GROWTH Russian patent published in 2006 - IPC A61K31/16 A61P35/00 

FIELD: organic chemistry, medicine, oncology, biochemistry, pharmacology.

SUBSTANCE: invention relates to the development of a method for inhibition in interaction of metalloproteinase 2 with integrin α_vβ₃ in host cells. Method involves contact of integrin with the amount of compound inhibiting this interaction and represented by the formula (I): wherein each of G¹ and G² represents 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; each of Y¹ and Y² represents independently -OH, (C₁-C₄)-alkyl, (C₁-C₄)-hydroxyalkyl, (C₁-C₄)-alkoxy-group, phenyl, benzyl or -NH₂; R¹ represents (C₁-C₄)-alkyl; each of X¹ and X² represents independently halogen atom or (C₁-C₄)-alkoxy-group; X³ represents halogen atom, nitro-group, (C₁-C₄)-alkyl, (C₁-C₄)-alkoxy-group or (C₁-C₄)-perfluoroalkyl; Z represents -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 represents hydrogen atom (H) or a covalent bond; each of m and n represents independently a whole number o or 1; t represents a whole number o or 1; each of p, r and v represents a whole number 1 or 2 and under condition that when A means hydrogen atom (H) then t is 0; when A means a covalent bond then t = 1, and when m = 0 then Y¹ represents (C₁-C₄)-hydroxyalkyl, and when n = o then Y² represents (C₁-C₄)-hydroxyalkyl. Also, invention describes a method for apoptosis induction involving administration of abovementioned substance in the therapeutically effective dose.

EFFECT: improved method for tumor inhibition, expanded assortment of antitumor agents.

37 cl, 9 dwg, 7 ex