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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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2002-10, Vol.12 (20), p.2931-2934
Main Authors: 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: Article
Language:English
Subjects:
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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Summary: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