- Abstract:
-
Alpha-halogenated analogues of the anti-resorptive bisphosphonate risedronate (5, Ris) and its phosphonocarboxylate cognate (7, 3-PEHPC) were synthesized and compared with 5, 7, and the corresponding desoxy analogues in bone mineral affinity and mevalonate pathway inhibition assays. The Ris (5e-h) and 3-PEHPC (7e-h) analogues had decreased bone mineral affinity, confirming that the alpha-OH group in 5 and 7 enhances bone affinity. The 5 alpha-halo-analogues potently inhibited farnesyl pyropho...
Expand abstract - Publication status:
- Published
- Publisher copy:
- 10.1021/jm0702884
-
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- Journal:
- Journal of medicinal chemistry
- Volume:
- 50
- Issue:
- 24
- Pages:
- 5967-5975
- Publication date:
- 2007-11-05
- DOI:
- EISSN:
-
1520-4804
- ISSN:
-
0022-2623
- URN:
-
uuid:614c8fca-0223-4157-95d6-c40937a79081
- Source identifiers:
-
107760
- Local pid:
- pubs:107760
- Language:
- English
- Keywords:
- Copyright date:
- 2007
Journal article
Synthesis and biological evaluation of alpha-halogenated bisphosphonate and phosphonocarboxylate analogues of risedronate.
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