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العنوان
Synthesis of new quinoline derivatives as potential anticancers and synthetic applications of diazonaphthoquinone /
المؤلف
Othman, Dina Ibrahim Ali.
هيئة الاعداد
باحث / دينا إبراهيم علي عثمان
مشرف / عاطف السيد طنطاوي
مشرف / ميتسورو كيتامورا
مشرف / ماجدة عبدالعزيز السيد
مشرف / خالد بشير شعبان سليم
الموضوع
Organic compounds. Quinoline.
تاريخ النشر
2018.
عدد الصفحات
258 p. :
اللغة
الإنجليزية
الدرجة
الدكتوراه
التخصص
علم السموم
تاريخ الإجازة
01/09/2018
مكان الإجازة
جامعة المنصورة - كلية الهندسة - Pharm. Org. Chemistry
الفهرس
Only 14 pages are availabe for public view

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from 258

Abstract

Fifty-four new compounds, that are not previously stated in any literature, were synthesized via six different schemes in the first part. All Reactions were monitored using TLC plates and the target compounds were purified either by silica gel column chromatography, preparative TLC or recrystallization. The structure elucidation of the new compounds was checked based on spectra analyses, IR, 1H NMR, 13C NMR, and high resolution mass spectrometry. All the newly synthesized compounds were subjected to MTT anticancer screening against human cell lines; breast adenocarcinoma (MCF-7), colon cancer (HCT-116), cervical epithelial cells (Hela), and hepatocellular carcinoma (HePG-2). Some promising compounds were selected for in vitro inhibition of Epidermal Growth Factors Receptor kinase (EGFR-TK) and topoisomerase II enzymes. In addition, some selected compounds were subjected to cell cycle analysis and apoptosis assay on MCF-7 cells. While in the second part, efforts on the development of the synthesis and application of diazonaphthoquinone chemistry were explained. In addition, the first total synthesis of Eleutherol and Eleuthoside A, the natural cytotoxic substances extracted from medicinal Indonesian plant, was accomplished via Rh-catalyzed intramolecular cyclization of the corresponding diazonaphthoquinone.