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
د / ممتاز السيد محمد بخيت | Momtaz El-sayed Mohamed Bakheet | 10796