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bsj-7978
Study of the Anticancer and Antimicrobial Biological Activity of a New Series of Thiohydantoin Derivatives
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        Recently, some prostate cancer patients have acquired resistance to the second -generation drugs (anzalutamide and apalutamide) prescribed for the treatment of this disease due to the emergence of the F876L mutation, which represents a challenge to modern medicine. In this study, a new series of 2-thiohydantoin derivatives were prepared through the reaction of different derivatives of maleimide (1c-4c) with isothiocyanate derivatives. The prepared compounds were diagnosed using FT-IR,1H-NMR ,13C-NMR, Mass spectra. The prepared series compounds has been studied against prostate cancer cells. The MTT assay was used to determine the activity of the prepared compounds against prostate cancer cells. The data indicated, depending on the IC50 values, that some of the prepared compounds have anti-prostate cancer activity. The results indicate that compounds 1d and 2d have good anti-prostate cancer activity compared to the rest of the compounds. The prepared series of compounds were also studied against selected types of bacteria and fungi, as the results showed that some of the compounds in the series had anti-bacterial and anti-fungal activity.

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Publication Date
Sat Jun 29 2024
Journal Name
Iraqi Journal Of Pharmaceutical Sciences( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis and Characterization of New 5-Fluoroisatin-Chalcone Conjugates with Expected Antimicrobial Activity
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Pathogenic microorganisms are becoming more and more resistant to antimicrobial agents. So the synthesis of new antimicrobial agents is very important. In this work, new 5-fluoroisatin-chalcone conjugates 5(a–g) were synthesized based on previous research that showed the modifications of the isatin moiety led to the synthesis of many derivatives that have antimicrobial activity. 4-aminoacetophenone reacts with 5-fluoroisatin to form Schiff base (3), which in turn reacts with two different groups of aromatic (carbocyclic and heterocyclic) aldehydes 4(a–g) separately to form the final compounds 5(a–g). Proton-nuclear magnetic resonance (¹H-NMR) and Fourier-transform infrared (FT-IR) spectroscopy were used to confirm the chemic

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Publication Date
Sun Sep 07 2014
Journal Name
Baghdad Science Journal
Study the effect of a new nikel (II) Complex and anticancer drug (cp) on Liver enzyme activity (GPT,GOT) and Creatinine level in Kidney of femal mice
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This study involved the effect of anew nickel (II) complexs with formla [NiL2(H2O)2].2.5ETOH where L=Bis[5-(p-nitrophenyL)-4-phenyL-1,2,4-traizole-3-dithocarbamato hydrazide] diaqua. nickel(II). Ethanol(2.5).and anti-cancer drug cyclophosphamide on specific actifity of two Liver enzymes (GOT,GPT) in the (Liver,kidney) tissues and on the creatinine Level in the kidney byUtilizing an invivosystem in femalmice.The result showed that inhibition in the activity of GPT and GOT enzymes in theLiver and in both nickel (II) complex and cyclophosphamide drug (CP) . mice weretreated with three doses (90,180,320) µg/mouse for three days for each group.The Liver show's the highest rate of GPT inhibition was about 97.43% at180µg/mouse regarding the ki

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Publication Date
Wed Sep 16 2020
Journal Name
Journal Of Chemistry
Synthesis of Phthalimide Imine Derivatives as a Potential Anticancer Agent
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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

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Publication Date
Thu Jun 25 2020
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis, Characterization and Antibacterial Activity Evaluation of New Indole-Based Derivatives
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A new series of N-acyl hydrazones (4a-g) derived from indole-3-propionic acid (IPA) were synthesized. These N-acyl hydrazones were prepared by the reaction of 3-(1H-indol-3-yl) propane hydrazide and aldehyde in the existence of glacial acetic acid as a catalyst. 1HNMR and FT-IR analyses were used to identify the synthesized compounds and they were in vitro evaluated as antibacterial agents against six different types of microorganisms by using well diffusion method. All the tested N-acyl hydrazones (4a-g) displayed moderate activity against the Gram-negative E.coli, comparable to that of Amoxicillin. Some of the tested N-acyl hydrazones also exhibited intermediate activity ag

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Publication Date
Tue Jun 05 2018
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis, Characterization and Alpha Glucosidase Inhibition activity of new Phthalimide Derivatives
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 Three of imide intermediate products  were synthesized by reacting of phthalic anhydride with glycine (2a), and tetrachloro phthalic anhydride with glycine , (S)-2-[(tert-Butoxycarbonyl)amino]-3-aminopropionic acid ( 2b,c)  respectively   in  dry toluene  with azeotropic removal of water using Dean- stark apparatus then carboxyl functional group activated by refluxing with  thionyl chloride, the resulted acid chloride (3a-c) were reacted with different amine (5-flourouracil, 4-chloroaniline, 4-bromoaniline, 2-amino thiazole, and pyrrolidine) (4a-e) , the   resulted products consider as

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Publication Date
Sun Aug 25 2024
Journal Name
University Of Samarra
Preparation, diagnosis and testing of the biological ‎activity of new complexes of Schiff bases
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‎ Sixteen new complexes with the general formula [M(L)2(H2O)2] were ‎prepared resulting from the reaction of the two new Schiff base ligands, which ‎are‏: -‏ L1= (E)-5-((2-hydroxybenzylidene)amino)-2-phenyl-2,4-dihydro-3H-pyrazol-3-one)‎ L2 = (E)-5-((2-hydroxy-3-methoxybenzylidene)amino)-2-phenylpyrazolidin-3-one) ‎ ‎ With divalent metal ions (manganese, cobalt, nickel, copper, zinc, cadmium, ‎mercury) and (tetravalent platinum).‎‏ ‏ ‎ Ligands was derived from the reaction of the amine (5-amino-2-phenyl-2,4-‎dihydro-3H-pyrazol-3-one) with Salicylaldehyde and ortho-vanillin, which is ‎linked to the metal ions via the nitrogen atoms are the isomethene group and ‎the oxygen is the hydroxide group of t

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Publication Date
Sat Nov 10 2018
Journal Name
Oriental Journal Of Chemistry
New Series of Substituted Heterocyclics Derived from α , β – Unsaturated Ketone and Their Cytotoxic Activity Tumor Cell Lines
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The aldol condensation of 2-acetylnaphthalene with 9-anthracene carboxaldehyde afforded α, β-unsaturated keton (1) . New heterocyclic compounds containing: cyclohexenone[2], indazole[3], pyrimidinethion [4], thiazolo fused pyrimidine[5], isoxazoline[6], substituted pyrazoline[7]a-d and pyrimidinone[8] rings system were synthesized from α, β-unsaturated keton[1]. Cyclization of [1] with ethylacetoacetate gave the mentioned heterocycle cyclohexanone [2]. The cyclo condensation of [2] with hydrazine gave the new indazole derivative [3]. furthermore, the reation of [1]with thiourea gives thiopyrmidine derivative [4]. The cyclo condensation of [4] with chloroacetic acid gave the fused rings [5]. Then reacted compound[1] with hydroxy

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Publication Date
Thu Jan 31 2019
Journal Name
Journal Of The College Of Education For Women
A New Vision in the Locality and the Factors of Forming Meander
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The research addressed an analytical field investigation of the locality of meander, the factors responsible of the locality of the meander at certain points of the stream other than others, and the role sequence of these factors in the formation process.
The research revealed that the location of forming the meander was associated closely with the scale structural composition of the bank materials from which the first stage of forming the curved stream, for the inhomogeneous or non-identical opposite banks in their scale structural composition saw an activity of differential corrosion, while the homogeneous and identical opposite banks in their scale structural composition saw an identical corrosion activity in its intensity at both

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Publication Date
Fri Jun 02 2017
Journal Name
Applied Organometallic Chemistry
A new azo‐Schiff base: Synthesis, characterization, biological activity and theoretical studies of its complexes
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A new Azo‐Schiff base ligand L was prepared by reaction of m‐hydroxy benzoic acid with (Schiff base B) of 3‐[2‐(1H–indol‐3‐yl)‐ethylimino]‐1.5‐dimethyl‐2‐phenyl‐2,3‐dihydro‐1H‐pyrazol‐4‐ylamine. This synthesized ligand was used for complexation with different metal ions like Ni(II), Co(II), Pd(II) and Pt(IV) by using a molar ratio of ligand: metal as 1:1. Resulted compounds were characterized by NMR (1H and 13C), UV–vis spectroscopy, TGA, FT‐IR, MS, elemental analysis, magnetic moment and molar conductivity studies. The activation thermodynamic parameters, such as ΔE*, ΔH*, ΔS*, ΔG*and

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Publication Date
Sun Dec 19 2021
Journal Name
International Journal Of Drug Delivery Technology
Synthesis and Characterization of New Compounds Derived from Amoxicillin and Evaluation of its Biological Activity
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Amoxicillin 1 was treated with thiosemicarbazide and Phosphoryl chloride to obtain a new derivatives that contains 1,3,4-thiadiazole moiety 2. Schiff bases compounds were synthesized by the reaction of compound 2 with different aldehydes such as benzaldehyde and some substituted Benzaldehyde; p-hydroy, p-Chloro, p-Nitro, p-Dimethylamino, p-Methyl, p-Methoxy, p-Ethoxy to give compounds 3a-h. The obtained compounds have tested towards gram -ve and gram +ve bacteria. The compound shows good to moderate result towards the bacteria.

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