Substituted uracil derivatives as potent inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1)

A new class of PARP-1 inhibitors, namely substituted fused uracil derivatives were synthesised. Starting from a derivative with an IC 50=2 μM the chemical optimisation program led to compounds with more than a 100-fold increase in potency (IC 50

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2002-11, Vol.12 (21), p.3187-3190
Hauptverfasser:	Steinhagen, Henning, Gerisch, Michael, Mittendorf, Joachim, Schlemmer, Karl-Heinz, Albrecht, Barbara
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Area Under Curve Biological and medical sciences Chemical Phenomena Chemistry, Physical Chromatography, High Pressure Liquid Drug Design Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacokinetics Enzyme Inhibitors - pharmacology Humans Indicators and Reagents Magnetic Resonance Spectroscopy Male Medical sciences Miscellaneous Pharmacology. Drug treatments Poly(ADP-ribose) Polymerase Inhibitors Rats Rats, Wistar Recombinant Proteins - antagonists & inhibitors Structure-Activity Relationship Uracil - analogs & derivatives Uracil - chemical synthesis Uracil - pharmacology
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Beschreibung
Zusammenfassung:	A new class of PARP-1 inhibitors, namely substituted fused uracil derivatives were synthesised. Starting from a derivative with an IC 50=2 μM the chemical optimisation program led to compounds with more than a 100-fold increase in potency (IC 50
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(02)00602-9