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العنوان
Design, synthesis and biological evaluation of heterocycles-based compounds as potential anti-tumor agents /
المؤلف
Nagi, Manar Ibrahim.
هيئة الاعداد
باحث / Manar Ibrahim Nagi
مشرف / Samia Mahmoud Mostafa
مشرف / Ismail Awadalla Salama
مشرف / khaled Darwish
الموضوع
Cancer. Indole. Benzimidazole.
تاريخ النشر
2020.
عدد الصفحات
119 p. :
اللغة
الإنجليزية
الدرجة
ماجستير
التخصص
الصيدلة ، علم السموم والصيدلانيات (المتنوعة)
تاريخ الإجازة
1/6/2020
مكان الإجازة
جامعة قناة السويس - كلية الصيدلة - كيمياء صيدلية
الفهرس
Only 14 pages are availabe for public view

from 119

from 119

Abstract

The present Thesis compromises the following chapters:
Chapter 1 (Introduction and literature review ):an introduction
describing cancer disease, its management, the role of BcL-2(Bcell
lymphoma-2) family in cancer management and its
inhibitors .
Chapter 2 (Scientific Rationale) :it describes how new drug
targeting BcL-2 protein can be designed
Chapter 3 (Results and Discussion): a correlation between the
chemical structures of novel compounds and obtained biological
activities, molecular docking studies, summery and conclusion.
Chapter 4 (experimental procedure):the present investigation
involves the synthesis of 14 final compounds
References : a list of references which were used and their
management according to their order in the thesis
Appendix: C13NMR and ,or H1NMR of all the compounds of
this work.
Apoptosis is a process of cellular suicide through which unwanted or unhealthy cells
are eliminated during organism development or cellular stress. Deregulated apoptosis
is a characteristic of cancer cells. The B-cell lymphoma-2 (Bcl-2) family plays pivotal
role in the mitochondrial pathway of apoptosis by promoting the release of
cytochrome c and Second mitochondrial-derived activator of caspases ( Smac) into
the cytosol, resulting in caspase-dependent cell death. In most tumor tissues and
cancer cell lines, the anti-apoptotic Bcl-2 proteins are frequently highly expressed.
For example, Bcl-2 is overexpressed in prostate cancer, breast cancer, B-cell
lymphomas, colorectal cancer. Therefore, developing potential inhibitors was an
important target to prove the significance of Bcl-2 in cancer recovery process. In the
present work, two schemes were designed, and new final compounds were
synthesized. Based on the suggested scaffolds, straightforward and convenient
synthetic chemical pathways were conducted as well as complete structural
elucidation of the obtained compounds was performed using 1H-NMR, 13C-NMR,
Mass spectrometry and elemental analysis. Concerning biological analysis, the
synthesized compounds were evaluated using breast cancer, human lung
adenocarcinoma, and non-malignant cell lines. Finally, molecular docking studies
have been adopted to examine the predicted binding mode for these final compounds
and obtain a greater insight through establishing SAR analysis correlating the
compound chemical structures and their in-vitro biological activities.