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Novel bisphosphonate inhibitors of the human farnesyl pyrophosphate synthase

โœ Scribed by Joris W. De Schutter; Serge Zaretsky; Sarah Welbourn; Arnim Pause; Youla S. Tsantrizos

Publisher
Elsevier Science
Year
2010
Tongue
English
Weight
687 KB
Volume
20
Category
Article
ISSN
0960-894X

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โœฆ Synopsis

A structure-based approach was pursued in designing novel bisphosphonate inhibitors of the human farnesyl pyrophosphate synthase (hFPPS). Preliminary SAR and structural evidence for the simultaneous binding of these inhibitors into the isopentenyl pyrophosphate (IPP) and the geranyl pyrophosphate (GPP) substrate sub-pockets of the enzyme are presented.

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A novel approach towards the synthesis o
A novel approach towards the synthesis of pyrophosphate analogues of farnesyl pyrophosphate
โœ A.R.P.M. Valentijn; O. van den Berg; G.A. van der Marel; J.H. van Boom; L.H. Coh ๐Ÿ“‚ Article ๐Ÿ“… 2010 ๐Ÿ› Elsevier Science ๐ŸŒ English โš– 415 KB

## Abstract The synthesis of two new analogues (__i.e.__ 3 and 4) of farnesyl pyrophosphate (FPP) containing a phosphonophosphate and a phosphonophosphonate moiety was accomplished via the phosphonomorpholidate. The latter was easily obtained by treatment of a phosphonic chloride with morpholine.