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العنوان
Synthesis, molecular modelling and biological evaluation of novel phthalazine and its bioisostere derivatives as potential anticancer agents /
الناشر
Wagdy Mohamed Mohamed Eldehna ,
المؤلف
Wagdy Mohamed Mohamed Eldehna
تاريخ النشر
2015
عدد الصفحات
186 Leaves :
الفهرس
Only 14 pages are availabe for public view

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from 251

Abstract

The discovery of efficacious new human therapeutic agents is one of humanity{u2019}s most vital tasks. It is an enormously demanding activity that requires creativity, a vast range of scientific knowledge, and great persistence. Cancer is one of the most difficult diseases to treat and it is a major disease responsible for deaths worldwide, it can be considered as one of the foremost health problems. Yet there is no cancer treatment that is 100% effective against disseminated cancer. Therefore, there is an urgent need to give much attention to update and modify drug leads to develop more potent and safe therapies. Encouraged by the marked anticancer activity exhibited by phthalazines and indolin-2-ones and the apparent role of VEGFR-2 inhibitors in the treatment of several tumors, it deemed of interest to design and synthesize novel series of 4- phenyl-1-(piperazin-1-yl)phthalazines, 4-(4-methoxybenzyl)phthalazines and 1-(4- ((2-oxoindolin-3-ylidene)amino)phenyl)-3-phenylureas as novel VEGFR-2 inhibitors and anticancer agents. The newly synthesized compounds were screened for their inhibitory activity against VEGFR-2 and their anticancer activity against different cell lines