2. Academic Validation
  3. 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

  • J Med Chem. 2005 Apr 21;48(8):2957-63. doi: 10.1021/jm040209d.
John M Sanders 1,  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
Affiliations

Affiliation

  • 1 Department of Chemistry, 600 South Mathews Avenue, University of Illinois at Urbana-Champaign, Urbana, Illinois 61801, USA.
PMID: 15828834 DOI: 10.1021/jm040209d
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.

Figures
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z