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تخليق مشتقات جديدة لمركبات اللاكتام و البريميدين و دراسة فعاليتها كمضادات للاكسدة و مضادات للاورام == Synthesis, Anti - Oxidant And Anti - Tumor Activity Of New Lactam And Pyrimidine Derivatives
Author name:
عبد الرحمن يسر خليفة الغزي
Supervisor name:
محمود شاكر مكطوف التميمي | حسام محمد كريديا
General topic:
Chemistry
Specific topic:
Organic Chemistry
Degree:
Doctorate
University:
University of Thi-Qar - College Of Science - Chemistry Department
Language:
English
University location:
Dhi Qar
Abstract:
In the end of last century the increasing of cancer disease has been speared in worldwide, has been pushing to investigate more in synthesis a new drug treatment herein, the idea in this thesis three types of heterocyclic compounds | were synthesized : | 1- Synthesis of a series of β-lactams 3(a-h) compounds by using Kinugasa reaction and Staudinger reaction, which β-lactam 3(a-b) compounds (as depicted in scheme below) were synthesized using Kinugasa reaction by reacting alkyne (phenylacetylene and 1-octyne) with the appropriate nitrones 2(a-b) in the presence triethylamine and CuI as catalyst and acetronitrel as solvent at 0˚C. R1 : 4-NHCOCH3 , 3-NO2 R2 : CH3(CH2) , 5 While β-lactam 3(c-h) compounds (as depicted in scheme below) were synthesized using Staudinger reaction by reacting methoxyacetyl chloride with the appropriate imines 2(c-h), in the presence of triethylamine in dry dichloromethane under nitrogen atmosphere at 0˚C.3c : R1= −C6H4Cl , R2= −C6H4− , 3f : R1= −C6H4Me , R2= −C6H4− | 3d : R1= −C6H4Br , R2= −C6H4− , 3g : R1= −C6H4Br , R2= −C6H4− 3e : R1= −C6H4Cl , R2= −C6H4− , 3h : R1= −C4H4N2 , R2= −C6H4− 2- Synthesis of a series of γ-lactams 4(a-h) (as depicted in scheme below) by reaction phenylsuccinic anhydride or 3-(4-chlorophenyl)dihydrofuran-2,5- dione with schiff bases (imines) 2(d,e,g,i,j,k,l,m), by using chloroform as solvent and heated at temperature (55-60˚C) Synthesis of a series of 3,4-Dihydropyrimidin-2(1H)-ones/ thiones 5(a-g) (as | depicted in scheme below) by reaction aldehyde, ethyl acetoacetate and | urea/thiourea under FeCl3.6H2O as catalyst, by using ethanol as solvent and heated at reflux temperature. | H2N NH2 | FeCl3.6H2O | ethanol , reflux | ethyl acetoacetate urea or thiourea aldehyde 5(a-g)The final products were characterized by using the basis of the spectral data : | IR, 1H-NMR, 13C-NMR and Mass. | The antioxidant activity for the synthesized compounds (3g, 4a, 5a) were examined and show highly biological activity response. Moreover, the activity against breast cancer MCF-7 cell line also studied and exhibited highly anti tumor.
