Quinone‐Fused Pyrazoles through 1,3‐Dipolar Cycloadditions: Synthesis of Tricyclic Scaffolds and in vitro Cytotoxic Activity Evaluation on Glioblastoma Cancer Cells

A novel and straightforward synthesis of highly substituted isoquinoline‐5,8‐dione fused tricyclic pyrazoles is reported. The key step of the synthetic sequence is a regioselective, Ag2CO3 promoted, 1,3‐dipolar cycloaddition of C‐heteroaryl‐N‐aryl nitrilimines and substituted isoquinoline‐5,8‐diones...

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Veröffentlicht in:	ChemMedChem 2018-09, Vol.13 (17), p.1744-1750
Hauptverfasser:	Bertuzzi, Giulio, Crotti, Simone, Calandro, Pierpaolo, Bonini, Bianca Flavia, Monaco, Ilaria, Locatelli, Erica, Fochi, Mariafrancesca, Zani, Paolo, Strocchi, Elena, Mazzanti, Andrea, Chiariello, Mario, Franchini, Mauro Comes
Format:	Artikel
Sprache:	eng
Schlagworte:	1,3-dipolar cycloaddition 1-Phosphatidylinositol 3-kinase anticancer drugs Anticancer properties Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Antineoplastic drugs Antitumor agents Aromatic compounds Benzoquinones - chemistry Benzoquinones - pharmacology Brain cancer Cancer Cell Line, Tumor Cell Proliferation - drug effects Cell Survival - drug effects Central Nervous System Neoplasms - drug therapy Central Nervous System Neoplasms - metabolism Central Nervous System Neoplasms - pathology Cycloaddition Cycloaddition Reaction Cytotoxicity Dose-Response Relationship, Drug Drug Screening Assays, Antitumor Functional groups Glioblastoma Glioblastoma - drug therapy Glioblastoma - metabolism Glioblastoma - pathology Humans Kinases Molecular docking Molecular Structure Phosphatidylinositol 3-Kinases - antagonists & inhibitors Phosphatidylinositol 3-Kinases - metabolism Protein Kinase Inhibitors - chemical synthesis Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Pyrazoles Pyrazoles - chemical synthesis Pyrazoles - chemistry Pyrazoles - pharmacology Quinones Scaffolds Signal Transduction - drug effects Structure-Activity Relationship Substitutes Synthesis TOR protein TOR Serine-Threonine Kinases - metabolism
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