National Institutes of Health, a Component of the US Dept. of Health & Human Services

Marek W Cholody

Christopher J Michejda

William G Rice

James A Turpin

Zoltan Szekely

Humcha Krishnamurthy Hariprakasha

A conjugate of formula: V&#x2014;(Y)&#x2014;Z-T: (I), T-X&#x2014;B&#x2014;(Y)&#x2014;Z-T': (II), V&#x2014;(Y)Z&#x2014;(Y&#x2032;)V&#x2032;: (III), T-X&#x2014;B&#x2014;(Y)&#x2014;Z&#x2014;(Y&#x2032;)&#x2014;X&#x2032;&#x2014;B&#x2032;-T&#x2032;: (IV), V&#x2014;(Y)&#x2014;Z&#x2014;(Y&#x2032;)&#x2014;X&#x2014;B-T: (V), V&#x2014;(Y)&#x2014;Z&#x2014;X&#x2014;B&#x2014;Z&#x2032;&#x2014;(Y&#x2032;)&#x2014;(V&#x2032;): (VI), or (W)&#x2014;(Y)&#x2014;[(Z)&#x2014;(Y&#x2032;)&#x2014;(X&#x2014;B)&#x2014;(Y&#x2033;)&#x2014;(Z&#x2032;)]&#x2014;(Y . . . )&#x2014;(W&#x2032;): (VII), in which W and W&#x2032; are independently a DNA intercalator or terminal subunit, V and V&#x2032; are independently a DNA intercalator, X and X&#x2032; are independently a DNA alkylator, B and B&#x2032; are the same or different and each is a heteoaromatic residue that is attached to the Nterminus of an alkylator subunit (X or X&#x2032;), Y, Y&#x2032;, Y&#x2033; and Y&#x2032;&#x2033; are independently a linker, T and T&#x2032; are independently terminal subunits, Z and Z&#x2032; 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.

DNA-binding polyamide drug conjugates

Acridone-derived compounds useful as antineoplastic and antiretroviral agents

The present invention relates to several novel acridone-derived compounds of of formula (I) or (II). These compounds are potent anti-viral agents, useful in the treatment of viral diseases, such as Human Immunodeficiency Virus. In addition, these compounds are anti-neoplastic agents useful in the treatment of various forms of cancer.

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Frederick, MD, United States of America

Marek W Cholody