Design, synthesis and biological evaluation of novel benzimidazoles / Sarah Hammad Mohamed Khairat ; Supervised Fatma Abdelfttah Ragab , Hoda Ibrahim Eldiwani
Material type:
- التصميم و التشييد و التقييم البيولوجى للبنزيميدازولات الجديده [Added title page title]
- Issued also as CD
Item type | Current library | Home library | Call number | Copy number | Status | Barcode | |
---|---|---|---|---|---|---|---|
![]() |
قاعة الرسائل الجامعية - الدور الاول | المكتبة المركزبة الجديدة - جامعة القاهرة | Cai01.08.05.Ph.D.2021.Sa.D (Browse shelf(Opens below)) | Not for loan | 01010110084365000 | ||
![]() |
مخـــزن الرســائل الجـــامعية - البدروم | المكتبة المركزبة الجديدة - جامعة القاهرة | Cai01.08.05.Ph.D.2021.Sa.D (Browse shelf(Opens below)) | 84365.CD | Not for loan | 01020110084365000 |
Browsing المكتبة المركزبة الجديدة - جامعة القاهرة shelves Close shelf browser (Hides shelf browser)
Thesis (Ph.D.) - Cairo University - Faculty of Pharmacy - Department of Pharmaceutical Chemistry
The present investigation deals with the synthesis of pyrazolylbenzimidazoles with bi substituents at both the benzimidazole and pyrazole moieties. All the synthesized compounds were tested for their ability to inhibit Sphingosine-1 kinase (SphK-1) which promotes tumor growth and is considered as a novel approach for treatment of cancer. Most of the tested compounds showed good percentage of inhibition. In addition, fluorescence binding studies of all the synthesized compounds was performed and compounds130,131, 138, 142, 144, 146,147, 148 and 150 revealed the formation of a stable protein-ligand complex. The IC50 of the nine compounds were calculated. In addition, the antiproliferative activity against 60 different cell lines were determined by NCI Development therapeutic program and the results showed that these compounds showed good inhibition percentage against different cell lines. Finally, molecular docking study was performed in the active site of SphK-1 to elucidate the mode of interaction
Issued also as CD
There are no comments on this title.