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العنوان
Green synthesis and biological activity evaluation of some novel thiazole-based heterocycles as potential anticancer agents /
الناشر
Doaa Zakaria Hassan Hassain ,
المؤلف
Doaa Zakaria Hassan Hassain
هيئة الاعداد
باحث / Doaa Zakaria Hassan Hassain
مشرف / Sobhy Mohamed Gomaa
مشرف / Hyam Abdelhamid Abdelhady
مشرف / Huda Kamel Mahmoud
تاريخ النشر
2021
عدد الصفحات
97 P. :
اللغة
الإنجليزية
الدرجة
ماجستير
التخصص
كيمياء المواد
تاريخ الإجازة
20/9/2020
مكان الإجازة
جامعة القاهرة - كلية العلوم - Organic Chemistry
الفهرس
Only 14 pages are availabe for public view

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from 117

Abstract

The original work of the submitted thesis consists of two new research projects entitled: (1) Microwave-assisted one-pot three component synthesis of some thiazolyl(hydrazonoethyl)thiazoles as potential anti-breast cancer agents and (2) Thiazole based thiosemicarbazones: synthesis, cytotoxicity evaluation and molecular docking study. In the first project: 1-(4-methyl-2-(2-(1-(thiophen-2-yl)ethylidene) hydrazinyl) thiazol-5-yl)ethanone was used as building block for synthesis of novel four series of 5-(1-(2-(thiazol-2-yl)hydrazono)ethyl) thiazole derivatives in a one-pot three-component reaction using both thermal heating and microwave irradiation for comparison.The bioactivities of the synthesized compounds were evaluated with respect to their antitumor activities against MCF-7 tumor cells in comparison with cisplatin reference drug using MTT assay. In the second project: 1-(4-Methyl-2-(2-(1-(thiophen-2-yl)ethylidene)hydrazinyl) thiazol-5-yl) ethanone was also used as building block for synthesis of novel series of 5-(1-(2-(thiazol-2-yl) hydrazono)ethyl) thiazole derivatives.The bioactivities of the synthesized compounds were evaluated with respect to their antitumor activities against MCF-7 tumor cells using MTT assay. Computer-aided docking protocol was performed to study the possible molecular interactions between the newly synthetic thiazole compounds and the active binding site of the target protein Rab7b. Moreover, the in silico prediction of adsorption, distribution, metabolism, excretion (ADME) and toxicity (T) properties of synthesized compounds were carried out using admet SAR tool