000			03175cam a2200349 a 4500
003			EG-GiCUC
005			20250223031904.0
008			171226s2017 ua h 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.2017.Na.D
100	0		_aNada Mosallam Mohamed Ghanem Mosallam
245	1	0	_aDesign, synthesis and biological evaluation of novel fused imidazo[4,5-b]pyridine derivatives as anticancer agents / _cNada Mosallam Mohamed Ghanem Mosallam ; Supervised Safinaz E. Abbas , Ossama M. Elbadry , Riham F. George
246	1	5	_aتصميم وتشييد وتقييم بيولوجي لمشتقات جديدة من الإيميداز و (4.5-ب) بيريدين كمضادات لمرض السرطان
260			_aCairo : _bNada Mosallam Mohamed Ghanem Mosallam , _c2017
300			_a135 P. : _bfacsimiles ; _c25cm
502			_aThesis (M.Sc.) - Cairo University - Faculty of Pharmacy - Department of Pharmaceutical Chemistry
520			_aCancer represents a major health problem. Although there has been a progress in the treatment and prevention of cancer, this disease remains the second major cause of death after cardiovascular diseases in the world. Accordingly, continued research is needed to develop new antitumor agents. Imidazopyridine scaffold had considerable therapeutic activities in the treatment of different cancer types such as breast, colon, glioma, prostate, colorectal and lung through inhibition of cyclin-dependent kinase enzymes (CDKs). Therefore, novel imidazopyridine were designed and synthesized starting from 4- (1H-imidazo[4,5-b]pyridin-2-yl)aniline I either via preparation of the diethyl methylene malonate derivative II followed by cyclization to pyrazolidine III-V, pyrimidine VI-VII, triazepine derivative VIII or diazotization of the amino functionality of I followed by coupling with phenol, aniline or active methylene derivatives to afford IXa-f, X and XI, respectively. The cytotoxic activity of the synthesized compounds was investigated against two cell lines, namely: MCF-7 and HCT-116. Compounds showing promising activity were further evaluated for their CDK9 inhibitory activity where they exhibited remarkable activity. Furthermore, molecular docking of the tested compounds was established with the active site of CDK9 enzyme domain to investigate the possible binding mode between the synthesized compounds and the binding pocket in the active site of the enzyme. In conclusion, based on both in vitro cytotoxicity study and CDK9 enzyme assay, most of the synthesized compounds exhibited significant anti-proliferative and CDK9 inhibitory activity, which suggests that these compounds might possible act as CDK9 inhibitors
530			_aIssued also as CD
653		4	_aAnticancer
653		4	_aCDK inhibitors
653		4	_aImidazo pyridine
700	0		_aOssama M. Elbadry , _eSupervisor
700	0		_aRiham F. George , _eSupervisor
700	0		_aSafinaz E. Abbas , _eSupervisor
856			_uhttp://172.23.153.220/th.pdf
905			_aNazla _eRevisor
905			_aShimaa _eCataloger
942			_2ddc _cTH
999			_c64259 _d64259