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العنوان
Design, synthesis and biological evaluation of novel 3-substituted quinoline derivatives as potential anti-cancer agents /
المؤلف
Mohamed, Basem Awad Mansour.
هيئة الاعداد
باحث / باسم عوض منصور
مشرف / محمد عادل محمود مسعود
مشرف / ماجدة عبد العزيز السيد
مشرف / وليد عبد الحكيم بيومي
مناقش / ماجدة عبد العزيز السيد
الموضوع
Quinoline. Pharmaceutical chemistry. Pharmacology. Organic compounds - Synthesis.
تاريخ النشر
2018.
عدد الصفحات
181 p. :
اللغة
الإنجليزية
الدرجة
الدكتوراه
التخصص
الصيدلة ، علم السموم والصيدلانيات
الناشر
تاريخ الإجازة
01/01/2018
مكان الإجازة
جامعة المنصورة - كلية الصيدلة - Department of Pharm. Org. Chemistry
الفهرس
Only 14 pages are availabe for public view

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Abstract

Surveying literature that shed light on the nature of the quinoline ring and other heterocyclic rings as anti-cancer, 45 final compounds were constructed in five different new series from which 36 new compounds not mentioned in literature before and assessed as anticancer on four types of cancer cells. The newly constructed compounds have been carefully analyzed and confirmed by IR, H NMR, C NMR,, MS and elemental analysis. The biological tests were conducted for all new compounds to detect their effectiveness as anti-cancer as well as their selectivity; the examined cancer cells were extracted from (breast, colon, liver and prostate). The biological evaluation of the new compounds was tested via MTT, ELISA and Water-LOGSY, and the effect of these compounds on cancer cells was studied and explained. from those NMR results, it’s clear that compound 118a is binding to ß-Catenin protein providing a promising possible ligand to inhibit the protein activity when overexpressed in tumors. The competition studies done by NMR is showing that compound 118a doesn’t compete with Tcf4 on the binding to ß-Catenin which can be justified based on the tighter binding between Tcf4/ ß-Catenin in comparison to compound 118a/ ß-Catenin complex.