A synthesis series of new heterocyclic derivatives (A2-A7) (pyrrole, pyridazine, oxazine and imidazol) derived from 4-acetyl-2,5-dichloro-1-(3,5-dinitrophenyl)-1H-pyrrole-3-carboxylate(A1) have been synthesised. Synthesis of compound (A2) by the reaction of starting material (A1) with hydroxyl amine hydrochloride in the presence of pyridine. Compound (A2) was reacted with hydrazine hydrate in dry benzene to give (A3) derivative. The compound )A3( deals with sodium nitrite to give diazonium salt, and the reaction diazonium salt with ethyl acetoacetate to produce compound (A4). To a mixture of compound (A4) and hydroxyl amine with sttired to yield (A5).Compound (A6) was prepared by reaction compound (A4) with thiosemicarbazide in presence of drops of acetic acid. Synthesis of 1compound (A7) by reaction compound (A6) with ethyl chloro acetate. The reactions have been monitored by TLC and the synthesized compounds were characterized using spectrophotometric methods FT-IR, 1H NMR.The biological effects of the prepared compounds on the cancer cells were studied in vitro. The results indicated that these Synthesized compounds (A1–A7) inhibited1 the cancer1 cells1 efficiently, the compound (A6) was activity inhibited on the cancer cells.
Synthesis, characterization and pharmaceutical studies of schiff base from 2-pyrrolidinone derivative and imidazole-2-carboxaldehyde and corresponding complexes with Metal (||)
The aim of this project was to study the in vitro effect of antineoplastic drugs (vincristine and vinblastine) on mice spermatozoa. Eighteen adult (age 8-9 weeks) male mice were divided into three groups equally. The animals in each group were slain by cervical dislocation, the testes were removed and two tails of epididymides isolated. Spermatozoa were obtained from the two tails of epididymides by mincing in 500 µl TCM-199.The first group non-treated (unadded) as a control group, second group added 10 µg/ml of vincristine to TCM-199 and the third group added 10 µg/ml of vinblastine to TCM-199. After 10 minutes from added of vincristine and vinblastin measured the following test: spermatozoa activity, percentage dead spermatozoa and mor
... Show MoreAll new compounds synthesized by many reactions starting from a product the compounds [I]a,b from reaction of 3-phenylenediamine or 4-phenylenediamine with chloroacetyl chloride, then the compounds [I]a,b reacted with potassium thiocyanate to yield compounds [II]a,b. While the compounds[III]a,b yield from reacted the compounds [I]a,b with sodium azide then the compounds [III]a,b reacted 1,3-dipolar cycloaddition reaction with acrylic acid to give compounds [IV]a,b and the later compounds reacted with phenylene diamine to product benzimidazole compounds [V]a,b . In addition to synthesized acid chloride compounds [VI]a,b by reacted the compounds [IV]a,b with thionyl chloride .Finally reacted the compounds [VI]a,b with different aromatic amine
... Show MoreMany previous investigations have found quercetin to be a powerful antioxidant and antitumor flavonoid, but its poor bioavailability has limited its use. This current study investigated the effects of two newly synthesized Quercetin Schiff bases containing 2-amino thiadiazole-5-thiol (Q1), and its benzyl derivatives (Q2) on MCF-7 human breast cancer cells. Cell viability and apoptosis were assessed to determine the toxic effects of Q1 and Q2. Cytotoxicity valuation showed that both compounds inhibited MCF-7 cell growth, and lactate dehydrogenase (LDH) activity increased in a dose-dependent aspect compared to the control group. Comet assay results observed that Q1 and Q2 induce more serious DNA damage than the control (untreated cell
... Show MoreA multistep synthesis was established for the preparation of a new vanillic acid-1, 2, 4-1triazole-3-thiol conjugate (
A new ligand [4-Methoxy -N-(pyrimidine-2-ylcarbamothioyl) benzamide] (MPB) was synthesized by reactioniofi(4-Methoxyibenzoyliisothiocyanate)withi(2-aminopyri-midine). The Ligand was characterized by elemental micro analysis (C.H.N.S),(FT-IR) (UV- Vis) and (1Hi,13CNMR)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 the obtained results the molecular formula of all complexes was suggested to be [M(MPB)2Cl2] (M+2i=Cu, Mn, Co ,Ni ,Zn ,Cd and Hg),the proposed geometrical structure for all complexes was an octahedral.
A new derivatives of Schiff bases connected with 5H-thiazolo[3,4-b][1,3,4]thiadiazole ring 5a-c were prepared via many reactions starting by treating 1,4-phenylene diamine 1 with chloroacetylchloride to prepared compound 2, then reaction with p-hydroxybenzaldehyde to synthesize compound 3 then, this was reacted with thioglycolic acid and thiosemicarazide to giveN,N-(1.4-phenylene)bis(2-(4-(2-amino-5Hthiazolo[4,3-b][1,3,4]thiadiazol-5-yl)phenoxy)acetamide) 4. Compound 4 was treated with different aromatic aldehydes to give a new derivatives of Schiff bases containing 5H-thiazolo[3,4-b][1,3,4]thiadiazole ring 5a-c. The synthesized compounds were characterized using FTIR spectrophotometer and 1H NMR spectroscopy and the biological activity of
... Show MoreThe Chemistry of heterocyclic sulphur and nitrogen containing compounds have a great role in the field of scientific studies, The 2-amino 5-mercapto-1,3,4-thiadiazole ring for instance, has gained more importance in recent years because they are considered as potent biologically active nucleus. In this study disulfide derivative can be obtained by oxidation with hydrogen peroxide of thiol group of the heterocyclic 2-amino 5-mercapto-1,3,4-thiadiazole ring to obtain compound (3) with expected antibacterial activity. In order to use it as a diazo component to prepare some new bis azo compounds as possible antibacterial agents, the reaction of two primary amino groups on both sides of disulfide dimer with sodium nitr
... Show MoreA series of metal ion complexes of some divalent transition metal ions having the general composition [ML2Cl2]nH2O with 2-(benzo[d]thiazol-2-ylamino)-2- (5-chloro-2-hydroxy phenyl) acetonitrile ligand has been prepared from 5-chloro-2-hydroxy-benzaldehyde and benzo[d]thiazol-2-amine. Existence of cyanide as potassium cyanide in acidic medium was considered, characterized by elemental chemical analysis, conductance of molarity, magnetic susceptibility measurements, FTIR electronic spectral studies and mole ratio method. FTIR indicates the participation of amino and acetonitrile nitrogen which is coordinated with the central metal ion.