Search In this Thesis
   Search In this Thesis  
العنوان
Design and Synthesis of Novel Quinoline Incorporating 1,2,4-Triazole Derivatives and Their Nitric Oxide Donor Analogues as Potential Anticancer and Anti-inflammatory Agents /
المؤلف
Mohassab, Aliaa Mohie El-Deen Othman.
هيئة الاعداد
باحث / علياء محي الدين عثمان محسب
مشرف / محمد عبد العزيز محمد عثمان
مشرف / هبة أحمد حسن
مشرف / داليا عبد الحميد سيد
الموضوع
Quinoline. Medicinal Chemistry.
تاريخ النشر
2017.
عدد الصفحات
194 p. :
اللغة
الإنجليزية
الدرجة
ماجستير
التخصص
الصيدلة ، علم السموم والصيدلانيات (المتنوعة)
تاريخ الإجازة
1/1/2017
مكان الإجازة
جامعة المنيا - كلية الصيدلة - كيمياء طبية
الفهرس
Only 14 pages are availabe for public view

from 219

from 219

Abstract

The introduced thesis deals with synthesis of two series of novel quinoline incorporating 1,2,4-triazole derivatives and their nitric oxide donor analogues in one compact structure for the purpose of synergistic activity as well as decreasing possible side effects produced from commonly used conventional NSAIDs. The synthesized derivatives were evaluated for their anti-cancer and anti-inflammatory activities as well as ulcerogenic liability. The introduced thesis includes various synthetic methodologies used for the preparation of 1,2,4-triazole derivatives as well as some of their biological activities, such as anti-malarial, anti-inflammatory, anti-cancer, anti-convulsant, and antifungal activities. The main goal of this thesis includes the incorporation of quinoline and 1,2,4-triazole rings as well as the oxime moeity as NO donor in one compact structure for the purpose of investigating the possible synergistic anti-cancer and anti-inflammatory activities and/or minimizing the gastric toxicity associated with classical NSAIDs. The synthesized compounds were evaluated for their ability to release NO under physiological conditions. The results showed that some of the synthesized compounds exhibited promising anticancer activity especially against melanoma and leukemia cancer cell lines as they were able to inhibit STAT3 phosphorylation which is involved in a wide variety of cancer types. Also most of the synthesized compounds showed remarkable anti-inflammatory activity relative to indomethacin as reference drug through selective inhibition towards COX-1 isozyme rather than COX-2 isozyme. The Synthesized compounds showed higher safety profile relative to indomethacin with normal tissue integrity.