A composition comprising an SL0101 [kaempferol 3-O-(3'',4''-di-O-acetyl-.alpha.-L-rhamnopyranoside)] derivative compound that has enhanced ability to inhibit RSK activity, relative to the parent compound is provided. The compounds have utility for treating any disease or conditions characterized or associated with excess or undesirable RSK activity. For example the RSK inhibitors of the present invention can be used to reduce the proliferation of neoplastic cells or for inhibiting the establishment or maintenance of an intracellular pathogenic infection by pathogens whose pathogenicity derives in part from the pathogen's ability to impede endosomal/phagosomal maturation in the host cell.

Hecht; Sidney M.

Lannigan-Macara; Deborah A.

Smith; Jeffrey Allan

O'Doherty; George A.

Hilinski; Michael Kenneth

University of Virginia Patent Foundation

Synthesis and identification of novel RSK-specific inhibitors

The present invention provides compositions and methods useful for preparing and using analogs, derivatives, and modifications of kaempferols that have anti-neoplastic activity. More specifically, the compounds are analogs, derivatives, and modifications of SLO1O1. The invention further provides compounds that are inhibitors of rsk activity. The invention further provides compounds that selectively inhibit excessive rsk activity in cancers. The present invention further provides methods for treating cancer using compounds of the invention.

kaempferol/kanser

Synthesis and identification of novel RSK-specific inhibitors

Rhamnose substituents of SL0101 and therapeutic uses thereof

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