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Lipophilic bisphosphonates

Experimentsl Therapeutics: Lipophilic Bisphosphonates Are Potent Inhibitors of Plasmodium Liver-Stage Growth

June 18, 2010 - 09:41 -- Kabogo Ndegwa
Agam Prasad Singh, Yonghui Zhang, Joo-Hwan No, Roberto Docampo, Victor Nussenzweig, and Eric Oldfield
Antimicrobial Agents and Chemotherapy, July 2010, p. 2987-2993, Vol. 54, No. 7

Nitrogen-containing bisphosphonates, drugs used to treat bone resorption diseases, also have activity against a broad range of protists, including blood-stage Plasmodium spp. Here, we show that new-generation "lipophilic" bisphosphonates designed as anticancer agents that block protein prenylation also have potent activity against Plasmodium liver stages, with a high (>100) therapeutic index.

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