DNA-binding polyamide drug conjugates

Details DNA-binding polyamide drug conjugates DNA-binding polyamide drug conjugates

2003-02-27

2009-10-20

Kosar, Andrew D. (Department: 1654)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

C514S002600, C424S001690

Reexamination Certificate

active

07605125

ABSTRACT:
A conjugate of formula: V—(Y)a—Z-T: (I), T-X—B—(Y)a—Z-T′: (II), V—(Y)aZ—(Y′)aV′: (III), T-X—B—(Y)a—Z—(Y′)a—X′—B′-T′: (IV), V—(Y)a—Z—(Y′)a—X—B-T: (V), V—(Y)a—Z—X—B—Z′—(Y′)a—(V′)b: (VI), or (W)a—(Y)b—[(Z)c—(Y′)d—(X—B)e—(Y″)f—(Z′)g]h—(Y . . . )i—(W′)j: (VII), in which W and W′ are independently a DNA intercalator or terminal subunit, V and V′ are independently a DNA intercalator, X and X′ are independently a DNA alkylator, B and B′ are the same or different and each is a heteoaromatic residue that is attached to the Nterminus of an alkylator subunit (X or X′), Y, Y′, Y″ and Y′″ are independently a linker, T and T′ are independently terminal subunits, Z and Z′ are independently a polyamide group that binds to the minor groove of DNA, a, b, c, d, f, g, i, and j are independently 0 to 5, and e and h are independently 1 to 5, a composition comprising a conjugate of any of formulae (I)-(VII) and a carrier, and a method for treating cancer in a mammal comprising administering an effective amount of a conjugate of any of formulae (I)-(VII) or a composition comprising same.

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