Design and synthesis of new quinoxaline derivatives as anticancer agents and apoptotic inducers

El Newahie A.M.S.; Nissan Y.M.; Ismail N.S.M.; Abou El Ella D.A.; Khojah S.M.; Abouzid K.A.M.

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Design and synthesis of new quinoxaline derivatives as anticancer agents and apoptotic inducers

El Newahie A.M.S.; Nissan Y.M.; Ismail N.S.M.; Abou El Ella D.A.; Khojah S.M.; Abouzid K.A.M.

Full Text link: https://t.ly/52XNY

Date issued: 2019

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Doi: https://doi.org/10.3390/molecules24061175 PubMed ID 30934622

Publisher: MDPI AG

Series Info: Molecules
24

Type: Article

Keywords: Anti-cancer activity , Cell cycle , Quinoxaline , Synthesis , antineoplastic agent , quinoxaline derivative , vasculotropin receptor 2 , antagonists and inhibitors , apoptosis , cell cycle checkpoint , cell proliferation , chemical structure , chemistry , dose response , drug design , drug effect , human , nuclear magnetic resonance spectroscopy , structure activity relation , synthesis , tumor cell line , Antineoplastic Agents , Apoptosis , Cell Cycle Checkpoints , Cell Line, Tumor , Cell Proliferation , Chemistry Techniques, Synthetic , Dose-Response Relationship, Drug , Drug Design , Humans , Magnetic Resonance Spectroscopy , Molecular Structure , Quinoxalines , Structure-Activity Relationship , Vascular Endothelial Growth Factor Receptor-2

Abstract:

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.