Design, synthesis, anticancer evaluation and molecular docking of new V600EBRAF inhibitors derived from pyridopyrazinone

• DOI: 10.5155/eurjchem.7.1.19-29.1346
• Publication Date: 2016-03-31T01:21:07Z
• Authors: Kamelia Mahmoud Amin; Ossama Metwally E...; Doaa Ezzat Abdel ...; Usama Magdi Ammar; Mohamed Mostafa A...
• Keywords: Docking (animal)

Design and synthesis of some new pyridopyrazinone derivatives as anti-proliferative agents is described. The cytotoxic activities the synthesized compounds against melanoma cell line (LOXIMVI), ovarian (OVCAR3), thyroid lines (CAL62, FTC133, BCPAP ML1) colon (HT29 HCT116) were investigated. Results revealed that most active compound 3d was one. It exhibited promising activity all tested lines. In addition, in vitro kinase assay both WT BRAF V600E performed for compounds. Furthermore, molecular docking established with site domain. inhibition that, 1, 3d, e, h, i, 5d, e 6b potent inhibitors enzyme involved number cancer types melanoma, cancer. newly pyridopyrazinones substituted different substituents at C-3 or fused triazine heterocycle C-4 afforded such ovarian,