عنوان المقالة: synthesis of novel 1, 2-bis-quinolinyl-1, 4-naphthoquinones: ERK2 inhibition, cytotoxicity and molecular docking studies
د / ممتاز السيد محمد بخيت | Momtaz El-sayed Mohamed Bakheet | 11026
- نوع النشر
- مجلة علمية
- المؤلفون بالعربي
- المؤلفون بالإنجليزي
- Ashraf A Aly, Essmat M El-Sheref, Momtaz EM Bakheet, Mai AE Mourad, Alan B Brown, Stefan Bräse, Martin Nieger, Mahmoud AA Ibrahim
- الملخص العربي
- Two novel series of N-2,3-bis(6-substituted-4-hydroxy-2-oxo-1,2-dihydroquinolin-3-yl)naphthalene-1,4-diones 3a-d and substituted N-(methyl/ethyl)bisquinolinone triethyl-ammonium salts 4e,f were successfully synthesized. The synthesized compounds were targeted as new candidates to extracellular signal-regulated kinases 1/2 (ERK1/2) with considerable antineoplastic activity. The synthesis involved the reactions of 2 equivalents of 4-hydroxy-2(1H)-quinolinones 1a-f and one equivalent of 1,4-naphthoquinone (2) in a mixture of ethanol/dimethylformamide (1:1) as a solvent and 0.5 mL Et3N. In the reaction of 6-methyl-4-hydroxyquinolone 1b with 2, a side product 4b of the second series was obtained. In general, the presence of free NH-quinolone gave a single compound of the first series, whereas reaction of N-methyl/ethyl-quinolones 1e,f with 2 enhanced the formation of compounds of the second series. The …
- تاريخ النشر
- 20/12/2018
- رقم المجلد
- رقم العدد
- رابط DOI
- https://doi.org/10.1016/j.bioorg.2018.09.017
- الكلمات المفتاحية
- 1,2-Bis-quinolinyl-1,4-naphthoquinones1,4-NaphthoquinoneCytotoxicityTargeting by ERK2Molecular docking