Pyrrolo[3,4-c]quinoline-1,3-diones as Potent Caspase-3 Inhibitors. Synthesis and SAR of 2-Substituted 4-Methyl-8-(morpholine-4-sulfonyl)-pyrrolo[3,4-c]quinoline-1,3-diones
| Autor: | Alexandre V. Ivachtchenko, Sergey E. Tkachenko, Ilya Okun, Dmitri V. Kravchenko, Volodymyr M. Kysil, Sergey Maliarchouk |
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| Rok vydání: | 2006 |
| Předmět: |
Stereochemistry
Drug Evaluation Preclinical Caspase 3 Quinolones Chemical synthesis Structure-Activity Relationship chemistry.chemical_compound Morpholine Drug Discovery Structure–activity relationship Enzyme Inhibitors IC50 Biological evaluation Pharmacology Sulfonyl chemistry.chemical_classification Molecular Structure biology Organic Chemistry Quinoline Stereoisomerism General Medicine Caspase Inhibitors Small molecule Sulfonamide Enzyme chemistry Enzyme inhibitor biology.protein |
| Zdroj: | ChemInform. 37 |
| ISSN: | 1522-2667 0931-7597 |
| DOI: | 10.1002/chin.200617150 |
| Popis: | Synthesis, biological evaluation and structure–activity relationships for a series of 2-substituted 4-methyl-8-(morpholine-4-sulfonyl)-1,3-dioxo-2,3-dihydro-1H-pyrrolo[3,4-c]quinolines are described. These compounds represent a new chemotype of nonpeptide small molecule inhibitors of caspase-3. Among the studied compounds, several potent inhibitors with IC50 in the range of 3–10 nM have been identified. The most active compound within this series, 7{49} and 7{58}, inhibited caspase-3 with IC50 = 3 nM. |
| Databáze: | OpenAIRE |
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