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العنوان
Design and synthesis of histone deacetylase inhibitors (HDACIs) as anticancer agents /
الناشر
Marwa Arafa Ibrahim Abdelaziz ,
المؤلف
Marwa Arafa Ibrahim Abdelaziz
هيئة الاعداد
باحث / Marwa Arafa Ibrahim Abdelaziz
مشرف / Samir Mohamed Elmoghazy
مشرف / Sahar Mahmoud Abouseri
مشرف / Riham Franc?ois George
تاريخ النشر
2020
عدد الصفحات
196 P. :
اللغة
الإنجليزية
الدرجة
الدكتوراه
التخصص
العلوم الصيدلية
تاريخ الإجازة
3/2/2020
مكان الإجازة
جامعة القاهرة - كلية الصيدلة - Pharmaceutical Chemistry
الفهرس
Only 14 pages are availabe for public view

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from 216

Abstract

In a search for new anticancer candidates, and motivated by the pivotal role of class III histone deacetylase (Sirtuins) in the occurrence and development of a variety of diseases including cancer, in addition to the promising anticancer activity exhibited by SIRT2 inhibitors, it deemed of interest to design and synthesize new series of phenolic azomethine derivatives and 5-arylidene thiazolidinones as novel anticancer SIRT2 inhibitors. In this regards, docking studies were performed to support the implemented design strategies. The synthesized target compounds were subjected to SITR2 enzyme inhibitory assay. Additionally, in vitro cytotoxic activities of the targeted compounds were tested in the NCI-60 human tumor cell line anticancer drug screening program, subsequently their selective cytotoxicity against the lung cancer cell line HOP-92 and the brain cancer cell line SNB-75 was assayed. Furthermore, the most active compounds were then tested for their effect on the cell cycle and apoptotic induction activity, in addition to their growth inhibitory activity against the human normal lung fibroblast cell line WI-38