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Synthesis and structure–activity relationships of novel poly(ADP-ribose) polymerase-1 inhibitors
- Source :
- Bioorganic & Medicinal Chemistry Letters. 16:938-942
- Publication Year :
- 2006
- Publisher :
- Elsevier BV, 2006.
-
Abstract
- A series of novel pyrrolocarbazoles was synthesized as potential PARP-1 inhibitors. Pyrrolocarbazole 1 was identified as a potent PARP-1 inhibitor (IC50 = 36 nM) from our internal database. Synthesis of analogs around this template with the aid of modeling studies led to the identification of the truncated imide 14. Compound 14 (IC50 = 40 nM), with deleted B-ring, was found to be an equipotent PARP-1 inhibitor.
- Subjects :
- Models, Molecular
Molecular model
Stereochemistry
Poly ADP ribose polymerase
Clinical Biochemistry
Carbazoles
Poly (ADP-Ribose) Polymerase-1
Pharmaceutical Science
Poly(ADP-ribose) Polymerase Inhibitors
Crystallography, X-Ray
Biochemistry
Chemical synthesis
Structure-Activity Relationship
chemistry.chemical_compound
Drug Discovery
Humans
Enzyme Inhibitors
Imide
Molecular Biology
chemistry.chemical_classification
Molecular Structure
biology
Organic Chemistry
NAD+ ADP-Ribosyltransferase
General Medicine
In vitro
Enzyme
chemistry
Enzyme inhibitor
biology.protein
Molecular Medicine
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 16
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....c35140b2fb10455bb87f2371800e7068