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العنوان
The Desigen,Synthesis & Biological Evaluation Of Novel Inhibitors Of The Anti-apoptotic Bcl-2 Protein /
المؤلف
Hussein, Rania Hamdy Ahmed Badawy.
هيئة الاعداد
باحث / Rania Hamdy Ahmed Badawy Hussein
مشرف / Mohamed El-Hoseny El-Sadek
مشرف / El-sayed Mansour Lashin
مشرف / Andrew West Well
الموضوع
Apoptosis- Molecular Aspects. Apoptosis Regulatory Proteins- Therapeutic Use.
تاريخ النشر
2013.
عدد الصفحات
260 P. :
اللغة
الإنجليزية
الدرجة
الدكتوراه
التخصص
الصيدلة ، علم السموم والصيدلانيات
تاريخ الإجازة
1/1/2013
مكان الإجازة
جامعة الزقازيق - كــليـــة الصيدلــــة - department of Pharmaceutical Chemistry
الفهرس
Only 14 pages are availabe for public view

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Abstract

Apoptosis isessential cellular process in the development and homeostasis of multicellular organisms. Defects in apoptosis pathways can promote cancer cell survival and also confer resistance to antineoplastic therapy. Over expression of anti-apoptotic Bcl2 family proteins in many types of human cancer has been associated with chemotherapy resistance. Preclinical studies have shown that agents targeting antiapoptotic Bcl-2 protein have preclinical activity as single agents or in combination with other antineoplastic agents. Bcl-2 is a promising molecular target for the design of a novel class of anticancer drugs aimed to overcome resistance of the cancer cell to apoptosis.
A structure based approach was employed to design novel small molecule anti-apoptotic Bcl-2 inhibitors in an attempt to understand the basic pharmacophore required for Bcl-2 inhibitory activity based on the lead compound 5-(1H-indol-3-yl)-N-(2-nitrophenyl)-1,3,4-oxadiazole-2-amine (6a) that previously obtained from virtual screening that found to be two fold less potent than gossypol in ELISA binding assay .