000 02313cam a2200337 a 4500
003 EG-GiCUC
005 20250223032825.0
008 211005s2021 ua h f m 000 0 eng d
040 _aEG-GiCUC
_beng
_cEG-GiCUC
041 0 _aeng
049 _aDeposite
097 _aPh.D
099 _aCai01.08.05.Ph.D.2021.Sa.D
100 0 _aSarah Hammad Mohamed Khairat
245 1 0 _aDesign, synthesis and biological evaluation of novel benzimidazoles /
_cSarah Hammad Mohamed Khairat ; Supervised Fatma Abdelfttah Ragab , Hoda Ibrahim Eldiwani
246 1 5 _aالتصميم و التشييد و التقييم البيولوجى للبنزيميدازولات الجديده
260 _aCairo :
_bSarah Hammad Mohamed Khairat ,
_c2021
300 _a158 P. :
_bfacsimiles ;
_c25cm
502 _aThesis (Ph.D.) - Cairo University - Faculty of Pharmacy - Department of Pharmaceutical Chemistry
520 _aThe 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
530 _aIssued also as CD
653 4 _aBiological evaluation
653 4 _aNovel benzimidazoles
653 4 _aSphingosine-1 kinase (SphK-1)
700 0 _aFatma Abdelfttah Ragab ,
_eSupervisor
700 0 _aHoda Ibrahim Eldiwani ,
_eSupervisor
856 _uhttp://172.23.153.220/th.pdf
905 _aNazla
_eRevisor
905 _aShimaa
_eCataloger
942 _2ddc
_cTH
999 _c82462
_d82462