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العنوان
SYNTHESIS OF NEW HETEROCYCLIC COMPOUNDS DERIVED from CYANOMEYTHYLENE AND β-DICARBONYLCOMPOUNDS AND THEIR CYTOTOXIC EVALUATION /
المؤلف
Elshehawy, Yasser Abdelaziz Ali.
هيئة الاعداد
باحث / ياسر عبد العزيز على الشهاوى
مشرف / خالد حسن حلمى
مناقش / رأفت ميلاد محارب
مناقش / خالد حسن حلمى
الموضوع
Chemistry, Organic. Carbon compounds.
تاريخ النشر
2018.
عدد الصفحات
246 p. :
اللغة
الإنجليزية
الدرجة
الدكتوراه
التخصص
Organic Chemistry
تاريخ الإجازة
2/10/2018
مكان الإجازة
جامعة المنوفية - كلية العلوم - قسم الكيمياء
الفهرس
Only 14 pages are availabe for public view

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Abstract

The reaction of cyclohexan-1,3-dione (1) with ethyl orthoformate (2) in acetic acid gave the 2-(ethoxymethylene) cyclohexane-1,3-dione (3). The latter compound was used for further heterocyclization reactions to give thiophene, thiophene, pyrazole and pyran derivatives. The cytotoxicity of the newly synthesized compound against the six cancer cell lines NUGC, DLDI, HA22T, HEPG2, HONE1 and MCF showed that compounds 5, 10c, 10d, 13b, 14a, 18b, 18d, 18e and 20b were the most potent compounds. On the other hand, the toxicity of these compounds against shrimp larvae indicated that compounds 7a, 10c, 13b, 14a, 18b and 18d were nontoxic against the tested organisms. Inhibition of the most potent compounds towards the tyrosine kinases c-kit, FIT-3, Vascular Endothelial Growth Factor Receptor (VEGFR)-2, Estimated Glomerular Filtration Rate (EGFR) and Platelet-Derived Growth Factor Receptor (PDGFR) revealed that compounds 5, 10c, 10d, 13b, 18b, 18d, 18e and 20b were of the highest inhibitory effect. The Pim-1 kinase test revealed that compounds 10d, 18b and 20b were of the highest inhibitory effect. In addition, the c-Met enzymatic activities showed that compounds 10c and 18b were the most potent compounds and their molecular docking was described.