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Design, synthesis, insilco study and biological evaluation of new isatin-sulfonamide derivatives by using mono amide linker as possible as histone deacetylase inhibitors
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Aim: To evaluate the cytotoxic activity of newly synthesized a series of novel HDAC inhibitors comprising sulfonamide as zinc binding group and Isatin derivatives as cap group joined by mono amide linker as required to act as HDAC inhibitors. Materials and Methods: The utilization of sulfonamide as zinc binding group joined by N-alkylation reaction with ethyl-bromo hexanoate as linker group that joined by amide reaction with Isatin derivatives as cap groups which known to possess antitumor activity in the designed of new histone deacetylase inhibitors and using the docking and MTT assay to evaluate the compounds. Results: Four compounds have been synthesized and characterized successfully by ART-FTIR, NMR and ESI-Ms. the compounds were synthesized and characterized by successfully by ART-FTIR, NMR and ESI- Ms. Assessed for their cytotoxic activity against human colon adenocarcinoma MCF-7 (IC50, I=105.15, II=60.00, III=54.11, IV=56.57, vorinostat=28.41) and hepatoblastoma HepG2 (IC50, I=63.91, II=135.18, III=118.85, IV=51.46, vorinostat=37.50). Most of them exhibited potent HDAC inhibitory activity and significant cytotoxicity. Conclusions: The synthesized compounds (I, II, III and IV) showed cytotoxicity toward MCF-7 and HepG2 cancer cell lines and their docking analysis provided a preliminary indication that they are viable [HDAC6] candidates.

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Publication Date
Fri Jan 01 2021
Journal Name
International Journal Of Pharmaceutical Research
New Polymeric Coii, Niii And Cdii Complexes With Tetrazole Schiff-Base Ligands; Synthesis, Spectral Characterisation And Biological Activity
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New Schiff-base ligands bearing tetrazole moiety and their polymeric metal complexes with Co(II), Ni(II) and Cd(II) ions are reported. Ligands were prepared in a multiple-step reaction. The reaction of sodium 2,6- diformylphenolate and cyclohexane-1,3-dione with 5-amino-2-fluorobenzonitrile resulted in the isolation of two precursors sodium 2,6-bis((E)-(3-cyano-4-fluorophenylimino)methyl)-4-methylphenolate 1 and 5,5'- (1E,1'E)-cyclohexane-1,3-diylidenebis- (azan-1-yl-1-ylidene)bis(2-fluorobenzonitrile) 2, respectively. The reaction of precursors with azide gave the required ligands; sodium 2,6-bis((E)-(4-fluoro-3-(1H-tetrazol-5- yl)phenylimino)methyl)-4-methylphenolate (NaL) and (N, N'E, N, N'E)-N, N'-(cyclohexane-1,3-diylidene)bis(4- fluor

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Publication Date
Sun Jan 01 2017
Journal Name
Al-mustansiriyah
Synthesis, Spectroscopic and Biological Studies of a New Some Complexes with N-Pyridin-2-Ylmethyl-Benzene-1, 2Diamine
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Publication Date
Sun Dec 01 2024
Journal Name
Indonesian Journal Of Chemistry
Synthesis, Characterization, Biological, and Antioxidant Activity of New Metal Ion Complexes with Schiff Base Derived from 2-Hydroxybenzohydrazide
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The study involved the synthesis of new complexes with tetradentate ligand (LH). The general formula of complexes was [M(LH)(H2O)2] with M of Ni2+, Co2+, Cu2+, and Zn+. The ligand was synthesized by treating the 2-hydroxybenzohydrazide with salicylaldehyde. The structural characteristics of ligands and complexes were analyzed using various techniques, including elemental analyses, magnetic susceptibility, molar conductivity, infrared, ultraviolet absorption, mass, and NMR spectroscopy studies. The physical measurements indicated that the prepared complexes are non-electrolyte and showed that the ligand is tetradentate when coordinated with metal ions through the nitrogen of azomethine (–C=N–), two oxygen atoms of O–H phenolic,

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Publication Date
Mon Aug 08 2022
Journal Name
Egyptian Journal Of Chemistry
Synthesis, Characterization, Spectroscopic, Thermal and Biological Studies for New Complexes with N1, N2-bis(3-hydroxyphenyl) Oxalamide
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Publication Date
Fri Jan 01 2021
Journal Name
Turkish Journal Of Physiotherapy And Rehabilitation
SYNTHESIS, SPECTROSCOPIC, CHARACTERIZATION AND BIOLOGICAL STUDIES FOR NEW COMPLEXES WITH N1, N5-BIS (3-HYDROXYPHENYL)- 2-OXOPENTANEDIAMIDE
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New complexes have been prepared from the new ligand [N1,N5-bis(3-hydroxyphenyl)-2- oxopentanediamide] derived from 2-Oxoglutaric acid and 3-aminophenol. Accordingly its binudear Mn(II),Co(II),Ni(II),Pd(II) and VO(II) complexes were prepared.. These compounds have been characterized by FT-IR, UV-Vis,Mass, 1H-NMR spectra, TGA curve, Chloride containing ,Molar conductance and atomic absorption. The characterization results gave binuclear complexes and pentadentate coordination and tetrahedral geometry for each Cobalt, Nickel, Manganese and Copper complexes otherwise Palladium complex gave a square planar geometry and Vanadium complex gave a square pyramidal geometry and the ligand is tetradentate. The biological activities for the new compoun

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Publication Date
Tue Mar 31 2020
Journal Name
College Of Islamic Sciences
The Origin of Creation in Khattab (The Beginning of Creation) by Imam Ali (as) and Genesis (Comparative Study)
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The research aims to answer the questions that revolve in the mind of mankind about how to create creation, how it existed prior to creation, who created existence, and the characteristics of that presence. The researcher also wanted to show that the culture of Imam Ali (peace be upon him) In the book of Adam, peace be upon him, God has punished Adam (peace be upon him) for not having sinned. Because his wife is the one who fed him the fruit of the tree, and this is contrary to what was stated in the sermon of Imam (peace be upon him) who Z Adam (peace be upon him) is the one who trusted Satan and Gwighth.

We note that the approach of the rhetoric has pointed to the creation of angels and did not refer to

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Publication Date
Tue Jan 14 2020
Journal Name
College Of Islamic Sciences
The Origin of Creation in Khattab (The Beginning of Creation) by Imam Ali (as) and Genesis (Comparative Study)
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The research aims to answer the questions that revolve in the mind of mankind about how to create creation, how it existed prior to creation, who created existence, and the characteristics of that presence. The researcher also wanted to show that the culture of Imam Ali (peace be upon him) In the book of Adam, peace be upon him, God has punished Adam (peace be upon him) for not having sinned. Because his wife is the one who fed him the fruit of the tree, and this is contrary to what was stated in the sermon of Imam (peace be upon him) who Z Adam (peace be upon him) is the one who trusted Satan and Gwighth.We note that the approach of the rhetoric has pointed to the creation of angels and did not refer to the creation of Eve and the class

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Publication Date
Thu May 15 2025
Journal Name
Chemchemtech
SYNTHESIS, CHARACTERIZATION AND SCREENING OF ANTIMICROBIAL ACTIVITY FOR SOME NEW SCHIFF BASES AND THIAZOLIDINONE DERIVATIVES DERIVED FROM AROMATIC CARBOXYLIC ACID
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In this study, the antimicrobial properties of newly synthesized Schiff bases (4a-4e) and thiazolidinone compounds (5a-5e) generated from 3,5-dinitrobenzoic acid were assessed. These compounds were obtained by reacting 3,5-dinitrobenzoic acid (1) with ethanol in a few drops of concentrated H2SO4 to produce the ester (2). The acid hydrazide (3), which was produced by treating the ester with hydrazine hydrate, reacted with the proper aldehydes, including 4-bromobenzaldehyde, 4-chlorobenzaldehyde, 4-hydroxybenzaldehyde, 4-methoxybenzaldehyde, and 4-hydroxy-3-methoxybenzaldehyde, respectively, to form Schiff bases (4a-4e). The thiazolidinone compounds (5a-5e) were produced by the cyclocondensation reaction of compounds (4a-4e) with thio

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Publication Date
Thu May 15 2025
Journal Name
Chemchemtech
SYNTHESIS, CHARACTERIZATION AND SCREENING OF ANTIMICROBIAL ACTIVITY FOR SOME NEW SCHIFF BASES AND THIAZOLIDINONE DERIVATIVES DERIVED FROM AROMATIC CARBOXYLIC ACID
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In this study, the antimicrobial properties of newly synthesized Schiff bases (4a-4e) and thiazolidinone compounds (5a-5e) generated from 3,5-dinitrobenzoic acid were assessed. These compounds were obtained by reacting 3,5-dinitrobenzoic acid (1) with ethanol in a few drops of concentrated H2SO4 to produce the ester (2). The acid hydrazide (3), which was produced by treating the ester with hydrazine hydrate, reacted with the proper aldehydes, including 4-bromobenzaldehyde, 4-chlorobenzaldehyde, 4-hydroxybenzaldehyde, 4-methoxybenzaldehyde, and 4-hydroxy-3-methoxybenzaldehyde, respectively, to form Schiff bases (4a-4e). The thiazolidinone compounds (5a-5e) were produced by the cyclocondensation reaction of compounds (4a-4e) with thio

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Publication Date
Thu May 14 2020
Journal Name
Journal Of Planner And Development
“The role of parametric approach in design highest climatic performance buildings: local housing design patterns as a sample”
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In light of increasing demand for energy consumption due to life complexity and its requirements, which reflected on architecture in type and size, Environmental challenges have emerged in the need to reduce emissions and power consumption within the construction sector. Which urged designers to improve the environmental performance of buildings by adopting new design approaches, Invest digital technology to facilitate design decision-making, in short time, effort and cost. Which doesn’t stop at the limits of acceptable efficiency, but extends to the level of (the highest performance), which doesn’t provide by traditional approaches that adopted by researchers and local institutions in their studies and architectural practices, limit

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