Journal article icon

Journal article

Synthesis, chiral high performance liquid chromatographic resolution and enantiospecific activity of a potent new geranylgeranyl transferase inhibitor, 2-hydroxy-3-imidazo[1,2-a]pyridin-3-yl-2-phosphonopropionic acid.

Abstract:

3-(3-Pyridyl)-2-hydroxy-2-phosphonopropanoic acid (3-PEHPC, 1) is a phosphonocarboxylate (PC) analogue of 2-(3-pyridyl)-1-hydroxyethylidenebis(phosphonic acid) (risedronic acid, 2), an osteoporosis drug that decreases bone resorption by inhibiting farnesyl pyrophosphate synthase (FPPS) in osteoclasts, preventing protein prenylation. 1 has lower bone affinity than 2 and weakly inhibits Rab geranylgeranyl transferase (RGGT), selectively preventing prenylation of Rab GTPases. We report here the ...

Expand abstract
Publication status:
Published

Actions


Access Document


Publisher copy:
10.1021/jm900232u

Authors


Expand authors...
Journal:
Journal of medicinal chemistry
Volume:
53
Issue:
9
Pages:
3454-3464
Publication date:
2010-05-05
DOI:
EISSN:
1520-4804
ISSN:
0022-2623
URN:
uuid:2a9bb265-c5b3-4000-ad02-79dd486f9181
Source identifiers:
107749
Local pid:
pubs:107749

Terms of use


Metrics


Views and Downloads






If you are the owner of this record, you can report an update to it here: Report update to this record

TO TOP