Browsing by Author "Khojah S.M."

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    Design and synthesis of new quinoxaline derivatives as anticancer agents and apoptotic inducers
    (MDPI AG, 2019) El Newahie A.M.S.; Nissan Y.M.; Ismail N.S.M.; Abou El Ella D.A.; Khojah S.M.; Abouzid K.A.M.; Pharmaceutical Organic Chemistry Department; Faculty of Pharmacy; October University for Modern Science and Arts (MSA); Cairo; 12611; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; Cairo University; Cairo; 11562; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; October University for Modern Science and Arts (MSA); Cairo; 12611; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmaceutical Sciences and Pharmaceutical Industries; Future University in Egypt; Cairo; 12311; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy Ain Shams University; Abbassia; Cairo 11566; Egypt; Department of Pharmaceutical Chemistry; Faculty of Pharmacy; Nahda University; Beni Suef; 62513; Egypt; Biochemistry Department; Faculty of Science; King Abdulaziz University; Jeddah; 21589; Saudi Arabia; Department of Organic and Medicinal Chemistry; Faculty of Pharmacy; University of Sadat City; Menoufia; 32897; Egypt
    The quinoxaline scaffold is a promising platform for the discovery of active chemotherapeutic agents. Three series of quinoxaline derivatives were synthesized and biologically evaluated against three tumor cell lines (HCT116 human colon carcinoma, HepG2, liver hepatocellular carcinoma and MCF-7, human breast adenocarcinoma cell line), in addition to VEGFR-2 enzyme inhibition activity. Compounds VIId, VIIIa, VIIIc, VIIIe and XVa exhibited promising activity against the tested cell lines and weak activity against VEGFR-2. Compound VIIIc induced a significant disruption in the cell cycle profile and cell cycle arrest at the G2/M phase boundary. In further assays, the cytotoxic effect of the highly active compounds was determined using a normal Caucasian fibroblast-like fetal lung cell line (WI-38). Compound VIIIc could be considered as a lead compound that merits further optimization and development as an anti-cancer and an apoptotic inducing candidate against the HCT116 cell line. � 2019 by the authors.