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  • Pyridinium-1-yl bisphosphonates are potent inhibitors of farnesyl diphosphate synthase and bone resorption.

Pyridinium-1-yl bisphosphonates are potent inhibitors of farnesyl diphosphate synthase and bone resorption.

Journal of medicinal chemistry (2005-04-15)
John M Sanders, Yongcheng Song, Julian M W Chan, Yonghui Zhang, Samuel Jennings, Thomas Kosztowski, Sarah Odeh, Ryan Flessner, Christine Schwerdtfeger, Evangelia Kotsikorou, Gary A Meints, Aurora Ortiz Gómez, Dolores González-Pacanowska, Amy M Raker, Hong Wang, Ermond R van Beek, Socrates E Papapoulos, Craig T Morita, Eric Oldfield
ABSTRACT

We report the design, synthesis and testing of a series of novel bisphosphonates, pyridinium-1-yl-hydroxy-bisphosphonates, based on the results of comparative molecular similarity indices analysis and pharmacophore modeling studies of farnesyl diphosphate synthase (FPPS) inhibition, human Vgamma2Vdelta2 T cell activation and bone resorption inhibition. The most potent molecules have high activity against an expressed FPPS from Leishmania major, in Dictyostelium discoideum growth inhibition, in gammadelta T cell activation and in an in vitro bone resorption assay. As such, they represent useful new leads for the discovery of new bone resorption, antiinfective and anticancer drugs.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Farnesyl pyrophosphate ammonium salt, methanol:ammonia solution, ≥95% (TLC)

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