New 4-amino-3-chloro benzoate ester derivatives as EGFR inhibitors: synthesis, in silico and biological analyses
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In the present study, ( Schiff's bases 6a - 6e) and (new amids derivatives 6f - 6j) have been synthesized . The glutaroyl chloride(2) has been prepared by the reacting of glutaric acid and thionyl chloride in presence of (DMF) . The new compound bis(4-formylphenyl) glutarate (3) has been Synthesized from reaction of one mole of glutaroyl chloride and two moles of 4-hydroxybenzaldehyde . Compound 4,4'-(glutaroylbis(oxy))dibenzoic acid (4) was Synthesized from one mole of glutaroyl chloride and two moles of 4-hydroxybenzoic acid, while compound bis(4-(chlorocarbonyl)phenyl) glutarate (5) was prepared from 4,4'-(glutaroylbis(oxy))dibenzoic acid and Thionyl chloride . Then Schiff's bases 6a - 6e that prepared
... Show MoreThis work include synthesized and characterization the compound [I] by reaction 1,4-phenylenediamine with chloro acetic acid then this compound reaction with methanol in present sulfuric acid to synthesized ester compound [II] after that reaction with hydrazine hydrate to synthesized acide hydrazide [III] and the later compound reaction with substituted acetophenone[IV]n to synthesized substituted acetophenone hydrazones[V-XI]. In addition synthesized4-formylpyrazole derivatives [XIIXVIII] via cyclisation substituted acetophenone hydrazones [V-XI] with Vilsmeier-Haack reagent DMF/POCl3. The compounds characterized by melting points, FTIR, 1HNMR and mass spectroscopy. The mesomorphic behavior studied by using polarized optical microscopy and
... Show MoreIn this work, prepared new ligand[3- (1H-indol-3-yl) -2- (3-(4- methoxybenzoyl)thiouereido) propanoic acid](MTP) has been synthesized by reaction of 4-Methoxybenzoyl isothiocyanate with tryptophane(1:1), The ligand was characterized by elemental microanalysis C.H.N.S, FT-IR, UV-Vis and 1H,13C NMR spectra, Some transition metals complexes of this ligand were prepared and characterized by FT-IR, UV-Vis spectra, conductivity measurements, magnetic susceptibility and atomic absorption, From obtained results the molecular formula of all prepared complexes were [M(MTP)2] (M+2 =Mn, Co, Ni, Cu, Zn, Cd and Hg), the proposed geometrical structure for all complexes were tetrahedral except copper complex has a square planer geometry around metallic ion
... Show MoreIn this work, the precursor [2-(1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-ylimino)acetic acid] was synthesised from 4-aminoantipyrine and glyoxylic acid, this precursor has been used in the synthesis of new multidentate ligand [2-((E)-3-(2-hydroxyphenylimino)-1,5-dimethyl-2-phenyl-2,3-dihydro-1H-pyrazol-4-ylimino)acetic acid][H2L] type (N2O2). The ligand was refluxed in ethanol with metal ions [VO(II), Mn(II), Co(II) and Ni(II)] salts to give complexes of general molecular formula:[M(H2L)2(X)(Y)].B, where: M=VO(II), X=0, Y=OSO3-2, B=2H2O; M=Mn(II),Co(II) ,X=Cl, Y=Cl, B=0; M=Ni(II), X=H2O, Y=Cl, B=Cl. These complexes were characterised by atomic absorpition(A.A), F.T-I.R., (U.V-Vis)spectroscopies (1H,13C NMR for ligand only), alon
... Show MoreNew complexes of Cu (ll), Ni (ll), Co (ll), and Zn (ll) wi th 2-amino-5-p-Fiouro Phenyl 1, 3, 4-Thiadiazole have been synthesized. The products were isolated, studied and characterized by physical measurements, ie,(Ff-IR), UV-Vis and the melting points were determined. The new Schiff base (L) has been used to prepare some complexes. The prepared complexes were identified and their structural geometry were suggested
Several new derivatives of 1, 2, 4-triazoles linked to phthalimide moiety were synthesized through following multisteps. The first step involved preparation of 2, 2-diphthalimidyl ethanoic acid [2] via reaction of two moles of phthalimide with dichloroacetic acid. Treatment of the resulted imide with ethanol in the second step afforded 2, 2-diphthalimidyl ester [3] which inturn was introduced in reaction with hydrazine hydrate in the third step, producing the corresponding hydrazide derivative [4]. The synthesized hydazide was introduced in different synthetic paths including treatment with carbon disulfide in alkaline solution then with hydrazine hydrate to afford the new 1, 2, 4-triazole [10]. Reaction of compound [10] with different alde
... Show Moresynthesis and characterization of New Bidentate schiff base Ligand Type(NO)Donor Atoms Derived from isatin and 3-Amino benzoic acid and Its complexes with Co(||),Cu(||),Cd(||)and Hg(||)Ions
The outstanding evidence of phthalimide pharmacophore in securing enhanced biological activities had encouraged further research and development into phthalimide-based derivatives as potential new drugs. In this study, phthalimide core was hybridized with aldehydes giving integrated imines displaying different types of functionalities and at alternating positions. The resulting compounds, therefore, provide an innovative window to explore possible differential biological effects as antioxidants and anticancer agents. A total of sixteen compounds were synthesized, and each was verified by FT-IR, H NMR, C NMR, and MS characterization. Herein, a facile single-step synthesis method was employed substituting the conventional two-step che
... Show MoreHeterocyclic polymers / silica nanocomposite one of important materials because of excellent properties such as thermal , electrical , and mechanical properties , so that hybrid nanomaterial are widely used in many fields, in this paper nanocomposite had prepared by modification of silica nanoparticals by using acrylic acid and functionalized the surface of nanoparticles, and using free Radical polymerization by AIBN as initiators and anhydrous toluene as solvent to polymerize functionalize silica nanoparticles with heterocyclic monomers to prepare heterocylic polymers / silica nanocomposite and study electrical conductivity , The nanocomposite which had prepared characterized by many analysis technique to study thermal properties such
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