Synthesis and biological evaluation of novel PDMP analogues

Synthesis and biological evaluation of novel PDMP analogues

A new series of hybrid PDMP analogues, based both on PDMP and styryl analogues of natural ceramide, has been synthesized from d-serine. The synthetic route was developed such that future introduction of different aryl groups is straightforward. Biological evaluation, both in vitro on rat liver Golgi...

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Veröffentlicht in:Bioorganic & medicinal chemistry 2006-08, Vol.14 (15), p.5273-5284
Hauptverfasser: Hillaert, Ulrik, Boldin-Adamsky, Swetlana, Rozenski, Jef, Busson, Roger, Futerman, Anthony H., Calenbergh, Serge Van
Format: Artikel
Sprache:eng
Schlagworte:
Animals
Biological and medical sciences
Cell Line
Cell Proliferation - drug effects
Cercopithecus aethiops
COS Cells
C–C coupling
Dose-Response Relationship, Drug
Drug Evaluation, Preclinical
Enzyme Inhibitors - chemical synthesis
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacology
Glucosylceramide synthase
Glucosyltransferases - antagonists & inhibitors
Golgi Apparatus - drug effects
Golgi Apparatus - enzymology
Humans
Inhibitor
Liver - drug effects
Liver - enzymology
Medical sciences
Miscellaneous
Molecular Structure
Morpholines - chemistry
Morpholines - pharmacology
PDMP
Pharmacology. Drug treatments
Rats
Sphingolipids
Structure-Activity Relationship
Subcellular Fractions - enzymology
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Beschreibung
Zusammenfassung:A new series of hybrid PDMP analogues, based both on PDMP and styryl analogues of natural ceramide, has been synthesized from d-serine. The synthetic route was developed such that future introduction of different aryl groups is straightforward. Biological evaluation, both in vitro on rat liver Golgi fractions as well as in HEK-293 and COS-7 cells, revealed two lead compounds with comparable inhibitory potency as PDMP, which could be elaborated to more potent inhibitors.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2006.03.048