دورية أكاديمية
Optimization of Aminoimidazole Derivatives as Src Family Kinase Inhibitors.
العنوان: | Optimization of Aminoimidazole Derivatives as Src Family Kinase Inhibitors. |
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المؤلفون: | Francini, Cinzia Maria, Musumeci, Francesca, Fallacara, Anna Lucia, Botta, Lorenzo, Molinari, Alessio, Artusi, Roberto, Mennuni, Laura, Angelucci, Adriano, Schenone, Silvia |
المصدر: | Molecules; Sep2018, Vol. 23 Issue 9, p2369, 17p, 8 Diagrams, 1 Chart |
مصطلحات موضوعية: | PROTEIN kinases, PHOSPHOTRANSFERASES, AMINOIMIDAZOLE ribonucleotide synthetase, PURINE synthesis, TYROSINE |
مستخلص: | Protein kinases have emerged as crucial targets for cancer therapy over the last decades. Since 2001, 40 and 39 kinase inhibitors have been approved by FDA and EMA, respectively, and the majority are antineoplastic drugs. Morevoer, many candidates are currently in clinical trials. We previously reported a small library of 4-aminoimidazole and 2-aminothiazole derivatives active as Src family kinase (SFK) inhibitors. Starting from these results, we decided to perform an optimization study applying a mix and match strategy to identify a more potent generation of 4-aminoimidazoles. Firstly, a computational study has been performed, then compounds showing the best predicted docking scores were synthesized and screened in a cell-free assay for their SFK inhibitory activity. All the new chemical entities showed IC |
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قاعدة البيانات: | Complementary Index |
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