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العنوان
Design, synthesis and biological evaluation of novel quinazoline derivatives and acyclic analogues as antineoplastic Agents /
الناشر
Ghada Fathy Hussien Elmasry ,
المؤلف
Ghada Fathy Hussien Elmasry
تاريخ النشر
2015
عدد الصفحات
146 P. :
الفهرس
Only 14 pages are availabe for public view

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from 163

Abstract

This work deals with the design and synthesis of some novel 6-iodo-2-(pyridin-3/4- yl)-3-substituted quinazolinone derivatives 8a-l, 10a-h, 13-18 in addition to certain acyclic analogues 9a-n and 12a-h. The in vitro cytotoxic activity of the synthesized compounds was performed against several cancer cell lines. Compounds eliciting superior cytotoxicity were further subjected to in vivo study. Kinase inhibitory assay was also carried out to investigate the mechanism of action of the target compounds and they displayed the highest activity against ABL kinase. Finally, a molecular modeling study was performed to figure out the interaction of some selected new compounds with the active site of ABL kinase