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008 191203s2019 ua 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.2019.Mo.S
100 0 _aMostafa Galal Eldin Elgazzar
245 1 0 _aSynthesis of some nitrogenous heterocyclic sulfonamide derivatives as anticancer and radiosensitizing agents /
_cMostafa Galal Eldin Elgazzar ; Supervised Fatma Abdelfattah Ragab , Helmy Ismail Heiba
246 1 5 _aتحضير بعض المركبات غير متجانسة الحلقة التى تحتوى على نواة النيتروجين و مجموعة السلفونميد كمضادات للأورام السرطانية و كمحفزات للأشعاع
260 _aCairo :
_bMostafa Galal Eldin Elgazzar ,
_c2019
300 _a159 P. ;
_c25cm
502 _aThesis (Ph.D.) - Cairo University - Faculty of Pharmacy - Department of Pharmaceutical Chemistry
520 _aIn a search for new cytotoxic agents with improved activity and selectivity, certain new N-pyridylsulfonamide derivatives have been synthesized. All the newly synthesized compounds were subjected to in vitro cytotoxic screening against human hepatocellular liver carcinoma cell line (HEPG2). The most potent compounds, as concluded from this screening, were selected to be evaluated for their in-vitro cytotoxic activity in combination with Þ-radiation. The new compounds were docked inside the active site of vascular endothelial growth factor receptor 2 (VEGFR2) kinase enzyme in an attempt to predict their mechanism of action and assayed for their inhibitory activity against VEGFR2. It has been concluded that 7 new synthesized compounds 11a, (5, 6)b and (10-13)b showed higher in-vitro cytotoxic activity against HEPG2 cell line than Sorafenib (IC50 range 0.12- 0.66 æM and IC50 for sorafenib = 1.06 æM), while the 3 newly synthesized compounds 5b, 11b and 12b are nearly equipotent to Sorafenib in decreasing the activity level of VEGFR2 kinase enzyme (IC50 33, 37 and 37 nM respectively and IC50 for sorafenib = 30 nM). Additionally the most 9 potent compounds showed a synergistic effect with radiation in the radiosensitizing evaluation, so the drug dose can be decreased and consequently the toxicity will be also decreased
530 _aIssued also as CD
653 4 _aAnticancer
653 4 _aPyridine
653 4 _aSulfonamide
700 0 _aFatma Abdelfattah Ragab ,
_eSupervisor
700 0 _aHelmy Ismail Heiba ,
_eSupervisor
856 _uhttp://172.23.153.220/th.pdf
905 _aNazla
_eRevisor
905 _aSamia
_eCataloger
942 _2ddc
_cTH
999 _c75631
_d75631