The United States of America, As Represented by the Secretary, Department of Health and Human Services

Laura K Cartner

Kirk R Gustafson

Michael C Dean

James Brislin McMahon

Susan Elaine Bates

Richard W Fuller

Curtis J Henrich

Heidi R Bokesch

Robert W Robey

Suneet Shukla

Suresh V Ambudkar

Kentaro Takada

Disclosed are methods of enhancing the chemotherapeutic treatment of tumor cells, reducing resistance of a cancer cell to a chemotherapeutic agent, a method of inhibiting ABCG2, Pgp, or MRP1 in a mammal afflicted with cancer, and a method of increasing the bioavailability of an ABCG2 substrate drug in a mammal. The methods comprise administering effective amounts of certain compounds to the mammal, for example, a compound of the formula (I): wherein R, R, R, X, X, X, a, and b are as described herein. Uses of these compounds in the preparation of a medicament are also disclosed. Also disclosed are compounds of formula (II), pharmaceutical compositions comprising such compounds and uses thereof.

Method of inhibiting ABCG2 and other treatment methods

Disclosed are methods of enhancing the chemotherapeutic treatment of tumor cells, reducing resistance of a cancer cell to a chemotherapeutic agent, a method of inhibiting ABCG2, Pgp, or MRP1 in a mammal afflicted with cancer, and a method of increasing the bioavailability of an ABCG2 substrate drug in a mammal. The methods comprise administering effective amounts of certain compounds to the mammal, for example, a compound of the formula (I): Formula (I), wherein R, R, R, X, X, X, a, and b are as described herein. Uses of these compounds in the preparation of a medicament are also disclosed. Also disclosed are compounds of formula (II), pharmaceutical compositions comprising such compounds and uses thereof. 

Botryllamides and method of inhibiting PGP in a mammal afflicted with cancer

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Middletown, MD, United States of America

Laura K Cartner