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Design, synthesis and biological screening of pyrazole and pyrazolopyrimidine derivatives as anticancer agents / Esraa Abdelmoneim Abdelmajeed Mostafa ; Supervised Ghaneya S. Hassan , Doaa E. Abdelrahman , Yassin M. Nissan

By: Contributor(s): Material type: TextTextLanguage: English Publication details: Cairo : Esraa Abdelmoneim Abdelmajeed Mostafa , 2017Description: 144 P. : photographs ; 25cmOther title:
  • تصميم و تشييد و مسح بيولوجى لمشتقات البيرازول و البيرازولوبيريميدين كمضادات للسرطان [Added title page title]
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Dissertation note: Thesis (M.Sc.) - Cairo University - Faculty of Pharmacy - Department of Pharmaceutical Chemistry Summary: Cancer is the second leading cause of death after cardiovascular complication with expectation of being first in coming few years. Accordingly, continued research is needed to develop new antitumor agents. Pyrazole or pyrazolopyrimidine scaffold is a very interesting bioactive core exhibiting several biological activities including anticancer, antimicrobial, antioxidant, antifungal and anti-inflammatory activities. In addition, sulfonamide functional moiety possessed good anticancer activity. Accordingly, new pyrazole or pyrazolopyrimidine derivatives bearing benzenesulfonamide moiety were designed and synthesized. The cytotoxic activities of the synthesized compounds against liver cancer cell line (HepG2) and breast cancer cell line (MCF7) were investigated. In addition, in vitro cell cycle analysis, apoptosis with its marker (caspase-3) and cyclin dependent kinase with its regulators (p21 and p27) were performed against the highly active compound to elucidate the possible mechanism of action. Furthermore molecular docking was established to predict the possible binding mode between the most active compound and the binding site in active site
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Item type Current library Home library Call number Copy number Status Date due Barcode
Thesis Thesis قاعة الرسائل الجامعية - الدور الاول المكتبة المركزبة الجديدة - جامعة القاهرة Cai01.08.05.M.Sc.2017.Es.D (Browse shelf(Opens below)) Not for loan 01010110072906000
CD - Rom CD - Rom مخـــزن الرســائل الجـــامعية - البدروم المكتبة المركزبة الجديدة - جامعة القاهرة Cai01.08.05.M.Sc.2017.Es.D (Browse shelf(Opens below)) 72906.CD Not for loan 01020110072906000

Thesis (M.Sc.) - Cairo University - Faculty of Pharmacy - Department of Pharmaceutical Chemistry

Cancer is the second leading cause of death after cardiovascular complication with expectation of being first in coming few years. Accordingly, continued research is needed to develop new antitumor agents. Pyrazole or pyrazolopyrimidine scaffold is a very interesting bioactive core exhibiting several biological activities including anticancer, antimicrobial, antioxidant, antifungal and anti-inflammatory activities. In addition, sulfonamide functional moiety possessed good anticancer activity. Accordingly, new pyrazole or pyrazolopyrimidine derivatives bearing benzenesulfonamide moiety were designed and synthesized. The cytotoxic activities of the synthesized compounds against liver cancer cell line (HepG2) and breast cancer cell line (MCF7) were investigated. In addition, in vitro cell cycle analysis, apoptosis with its marker (caspase-3) and cyclin dependent kinase with its regulators (p21 and p27) were performed against the highly active compound to elucidate the possible mechanism of action. Furthermore molecular docking was established to predict the possible binding mode between the most active compound and the binding site in active site

Issued also as CD

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