000			02894cam a2200325 a 4500
003			EG-GiCUC
008			190127s2018 ua dh f m 000 0 eng d
040			_aEG-GiCUC _beng _cEG-GiCUC
041	0		_aeng
049			_aDeposite
097			_aM.Sc
099			_aCai01.08.05.M.Sc.2018.Me.S
100	0		_aMennatullah Nagy Abdelhamed
245	1	0	_aSynthesis of certain 1,3,5-trisubstituted pyrazole derivatives of potential anticancer activity / _cMennatullah Nagy Abdelhamed ; Supervised Safinaz Elsayed Abbas , Riham François George , Eman Mohamed Samir
246	1	5	_aتشييد بعض مشتقات 1, 3, 5- ثلاثي مستبدلات البيرازول المتوقع لها فاعلية مضادة للسرطان
260			_aCairo : _bMennatullah Nagy Abdelhamed , _c2018
300			_a111 P. : _bcharts , facsimiles ; _c25cm
502			_aThesis (M.Sc.) - Cairo University - Faculty of Pharmacy - Department of Pharmaceutical Chemistry
520			_aCancer is the second cause of mortality after cardiac diseases in the world. It is continuing to act as a major problem of health in both developing and developed countries. Therefore, there is a continuous need to search of new anticancer hits that inhibit different targets leading to more efficacies and less side effects compared to the traditional agents.Literature cited that pyrazoleand pyrazoline derivatives display a therapeutic activity as anticancer agents against breast, colon, lung, liver, cervical cancer by acting on variable targets through different mechanisms of action.Accordingly, the present study is concerned with the synthesis of new derivatives belonging to 1,3,5-trisubstituted pyrazole/pyrazolinesVIa,b,VII, VIIIand substituted thiazolylpyrazolinesXa-d, XIIa-c,XIVa-d. This is achieved via two intermediates, namely: 2-chloro-6-methoxy quinolin-3-yl chalcone IV and 5-(2-chloro-6-methoxyquinolin-3-yl)-3-(p-tolyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide VIb. The newly synthesized compoundswere evaluated for their in vitro cytotoxicity against three human cancer cell lines namely: MCF7 (breast), Hela (cervical), DLD1 (colon) in addition to normal fibroblast cell (WI38) relative to CHS 828 as a reference compound. Compounds eliciting superior anticancer activity were screened their EGFR inhibitory activity compared to gefitinib.Moreover a molecular docking study was performed on compounds exhibiting significant EGFR inhibitory activity to find their binding mode in the active site of the enzyme
530			_aIssued also as CD
653		4	_a1,3,5-trisubstituted pyrazole
653		4	_aAnticancer
653		4	_aCancer
700	0		_aEman Mohamed Samir , _eSupervisor
700	0		_aRiham François George , _eSupervisor
700	0		_aSafinaz Elsayed Abbas , _eSupervisor
905			_aNazla _eRevisor
905			_aShimaa _eCataloger
942			_2ddc _cTH
999			_c69775 _d69775