Publication number: 20090069220
Abstract: A conjugate of formula: V—(Y)a-Z-T??(I), T-X—B—(Y)a-Z-T???(II), V—(Y)a-Z-(Y?)a—V???(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 heteroaromatic residue that is attached to the N-terminus 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
Type:
Application
Filed:
September 16, 2008
Publication date:
March 12, 2009
Applicant:
GOVERNMENT OF THE UNITED STATES OF AMERICA, REPRESENTED BY THE SECRETARY, DEPA
Inventors:
Zoltan Szekely, Humcha Krishnamurthy Hariprakasha, Marek W. Cholody, Christopher Michejda