Browsing by Author "Abouzid K.A.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.
Discovery of new HER2/EGFR dual kinase inhibitors based on the anilinoquinazoline scaffold as potential anti-cancer agents
(Informa Healthcare, 2014) Sadek M.M.; Serrya R.A.; Kafafy A.-H.N.; Ahmed M.; Wang F.; Abouzid K.A.M.; Department of Pharmaceutical Organic Chemistry; Faculty of Pharmacy; MSA University; 6th October; Cairo; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; Ain Shams University; Cairo 11566; Egypt; Pharmaceutical Organic Chemistry Department; Faculty of Pharmacy; Assiut University; Abbassia; Cairo; Egypt; Chemistry Laboratory; Faculty of Life and Social Sciences; Swinburne University of Technology; Melbourne; VIC; Australia
Herein, we designed and synthesized certain anilinoquinazoline derivatives bearing bulky arylpyridinyl, arylpropenoyl and arylpyrazolyl moieties at the 4? position of the anilinoquinazoline, as potential dual HER2/EGFR kinase inhibitors. A detailed molecular modeling study was performed by docking the synthesized compounds in the active site of the epidermal growth factor receptor (EGFR). The synthesized compounds were further tested for their inhibitory activity on EGFR and HER2 tyrosine kinases. The aryl 2-imino-1,2-dihydropyridine derivatives 5d and 5e displayed the most potent inhibitory activity on EGFR with IC50 equal to 2.09 and 1.94 ?M, respectively, and with IC50 equal to 3.98 and 1.04 ?M on HER2, respectively. Furthermore, the anti-proliferative activity of these most active compounds on MDA-MB-231 breast cancer cell lines, known to overexpress EGFR, showed an IC50 range of 2.4 and 2.5 ?M, respectively. � 2014 Informa UK Ltd. All rights reserved.
Quinoxaline-Based Scaffolds Targeting Tyrosine Kinases and Their Potential Anticancer Activity
(Wiley-VCH Verlag, 2016) El Newahie A.M.S.; Ismail N.S.M.; Abou El Ella D.A.; Abouzid K.A.M.; Faculty of Pharmacy; Department of Pharmaceutical Organic Chemistry; October University for Modern Science and Arts (MSA); Cairo; Egypt; Faculty of Pharmaceutical Sciences and Pharmaceutical Industries; Department of Pharmaceutical Chemistry; Future University; Cairo; Egypt; Faculty of Pharmacy; Department of Pharmaceutical Chemistry; Ain Shams University; Abbassia; Cairo; 11566; Egypt
Quinoxaline derivatives, also called benzopyrazines, are an important class of heterocyclic compounds. Quinoxalines have drawn great attention due to their wide spectrum of biological activities. They are considered as an important basis for anticancer drugs due to their potential activity as protein kinase inhibitors. In this review, we focus on the chemistry of the quinoxaline derivatives, the strategies for their synthesis, their potential activities against various tyrosine kinases, and on the structure-activity relationship studies reported to date. � 2016 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.