Novel guanidine-based inhibitors of inosine monophosphate dehydrogenase

A series of novel guanidine-based small molecule inhibitors of inosine monophosphate dehydrogenase (IMPDH) was explored. IMPDH catalyzes the rate determining step in guanine nucleotide biosynthesis and is a target for anticancer, immunosuppressive and antiviral therapy. The synthesis and the structu...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2002-10, Vol.12 (20), p.2931-2934
Hauptverfasser:	IWANOWICZ, Edwin J, WATTERSON, Scott H, HOLLENBAUGH, Diane L, CHUNJIAN LIU, GU, Henry H, MITT, Toomas, LEFTHERIS, Katerina, BARRISH, Joel C, FLEENER, Catherine A, ROULEAU, Katherine, SHERBINA, N. Z
Format:	Artikel
Sprache:	eng
Schlagworte:	Antineoplastic agents Antiviral Agents - chemical synthesis Antiviral Agents - pharmacology Biological and medical sciences Crystallography, X-Ray Dose-Response Relationship, Drug Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology General aspects Guanidine - analogs & derivatives Guanidine - chemical synthesis Guanidine - pharmacology Humans IMP Dehydrogenase - antagonists & inhibitors Indicators and Reagents Medical sciences Pharmacology. Drug treatments Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	A series of novel guanidine-based small molecule inhibitors of inosine monophosphate dehydrogenase (IMPDH) was explored. IMPDH catalyzes the rate determining step in guanine nucleotide biosynthesis and is a target for anticancer, immunosuppressive and antiviral therapy. The synthesis and the structure-activity relationships (SARs), derived from in vitro studies, for this new series of inhibitors is given.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(02)00600-5