Search Results - "Aboraia, Ahmed S."
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Synthesis, computational study and biological evaluation of 9-acridinyl and 1-coumarinyl-1,2,3-triazole-4-yl derivatives as topoisomerase II inhibitors
Published in Journal of enzyme inhibition and medicinal chemistry (01-12-2022)“…Topoisomerase (IIB) inhibitors have been involved in the therapies of tumour progression and have become a major focus for the development of anticancer…”
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Utilization of tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidinone as a cap moiety in design of novel histone deacetylase inhibitors
Published in Bioorganic chemistry (01-10-2019)“…[Display omitted] •12 novel compounds contain Tetrahydrobenzo[4,5]Thieno[2,3-d]pyrimidinone as a novel cap group, attached to ZBG via aliphatic, aralkyl or…”
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3
Effects of Lidocaine-Derived Organic Compounds on Eosinophil Activation and Survival
Published in Molecules (Basel, Switzerland) (27-07-2023)“…Lidocaine, a local anesthetic, is known to possess anti-inflammatory properties. However, its clinical use is limited by inconveniences, such as its local…”
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Bioactive fluorenes. Part III: 2,7-dichloro-9H-fluorene-based thiazolidinone and azetidinone analogues as anticancer and antimicrobial against multidrug resistant strains agents
Published in BMC chemistry (25-06-2020)“…Background Thiazoles, thiazolidinones and azetidinones are highly ranked amongst natural and synthetic heterocyclic derivatives due to their great…”
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N4-Substituted Piperazinyl Norfloxacin Derivatives with Broad-Spectrum Activity and Multiple Mechanisms on Gyrase, Topoisomerase IV, and Bacterial Cell Wall Synthesis
Published in ACS bio & med chem au (20-12-2023)“…Fluoroquinolones are an important class of antibiotics with broad-spectrum antibacterial and antitubercular activity. Here, we describe the design and…”
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Anti-Allergic and Anti-Inflammatory Effects of Lidocaine-Derived Organic Compounds in a House Dust Mite-Induced Allergic Rhinitis Mouse Model
Published in Biomedicines (29-08-2024)“…Allergic rhinitis (AR) is a common chronic disease that significantly impacts the quality of life. Lidocaine is known to have anti-inflammatory and…”
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Design, Synthesis, Molecular Modeling, Biological Activity, and Mechanism of Action of Novel Amino Acid Derivatives of Norfloxacin
Published in ACS omega (14-11-2023)“…Two series of N4-substituted piperazinyl amino acid derivatives of norfloxacin (24 new compounds) were designed and synthesized to attain structural surrogates…”
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Small Molecule Inhibitors of Retinoic Acid 4-Hydroxylase (CYP26): Synthesis and Biological Evaluation of Imidazole Methyl 3-(4-(aryl-2-ylamino)phenyl)propanoates
Published in Journal of medicinal chemistry (28-04-2011)“…The synthesis and potent inhibitory activity of novel imidazole methyl 3-(4-(aryl-2-ylamino)phenyl)propanoates in a MCF-7 CYP26A1 microsomal assay is…”
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Synthesis, theoretical investigations, biocidal screening, DNA binding, in vitro cytotoxicity and molecular docking of novel Cu (II), Pd (II) and Ag (I) complexes of chlorobenzylidene Schiff base: Promising antibiotic and anticancer agents
Published in Applied organometallic chemistry (01-12-2018)“…Three new Cu (II), Pd (II) and Ag (I) complexes of bidentate Schiff base ligand 2‐[(4‐chlorobenzylidene)amino] phenol (HL) were synthesized. The stoichiometric…”
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Design, synthesis, and antibacterial evaluation of new quinoline-1,3,4-oxadiazole and quinoline-1,2,4-triazole hybrids as potential inhibitors of DNA gyrase and topoisomerase IV
Published in Bioorganic chemistry (01-07-2021)“…[Display omitted] •A series of novel quinoline-1,3,4-oxadiazole and quinoline-1,2,4-triazole hybrids has been designed and synthesized.•The new hybrids were…”
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Fatty Acid Conjugated Chalcones as Tubulin Polymerization Inhibitors: Design, Synthesis, QSAR, and Apoptotic and Antiproliferative Activity
Published in Journal of natural products (Washington, D.C.) (26-05-2023)“…Cancer is often associated with an aberrant increase in tubulin and microtubule activity required for cell migration, invasion, and metastasis. A new series of…”
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Design, synthesis and pharmacophoric model building of new 3‐alkoxymethyl/3‐phenyl indole‐2‐carboxamides with potential antiproliferative activity
Published in Chemical biology & drug design (01-07-2017)“…Novel 3‐alkoxymethyl/3‐phenyl indole‐2‐carboxamide derivatives were synthesized and evaluated for their anticancer activity. Most of the tested compounds…”
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Synthesis, characterization, molecular modeling studies, and biological evaluation of metal piroxicam complexes (M = Ni(II), Pt(IV), Pd(II), Ag(I)) as antibacterial and anticancer agents
Published in Drug development research (01-04-2024)“…Four piroxicam metal complexes; NiL2, PtL2, PdL2, and AgL were synthesized and characterized by different techniques with enhanced antibacterial and anticancer…”
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Design, synthesis, docking studies and biological evaluation of novel chalcone derivatives as potential histone deacetylase inhibitors
Published in Bioorganic chemistry (01-06-2017)“…[Display omitted] •Chalcone derivatives comprising hydroxamic acids or 2-aminobenzamide as zinc binding groups.•Anti-proliferative activity against human…”
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Design, synthesis and evaluation against Mycobacterium tuberculosis of azole piperazine derivatives as dicyclotyrosine (cYY) mimics
Published in Bioorganic & medicinal chemistry (01-01-2018)“…[Display omitted] Three series of azole piperazine derivatives that mimic dicyclotyrosine (cYY), the natural substrate of the essential Mycobacterium…”
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Novel 5-(2-hydroxyphenyl)-3-substituted-2,3-dihydro-1,3,4-oxadiazole-2-thione derivatives: Promising anticancer agents
Published in Bioorganic & medicinal chemistry (15-02-2006)“…A series of 5-(2-hydroxyphenyl)-3-substituted-2,3-dihydro-1,3,4-oxadiazole-2-thione derivatives was synthesized and tested for anticancer activity. A series of…”
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Small-Molecule Inhibitors of 25-Hydroxyvitamin D‑24-Hydroxylase (CYP24A1): Synthesis and Biological Evaluation
Published in Journal of medicinal chemistry (25-09-2014)“…The synthesis of imidazole styrylbenzamide, tert-butyl styrylimidazole, and tert-butyl styrylsulfonate derivatives is described. Evaluation of binding…”
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Design, synthesis and antiproliferative evaluation of lipidated 1,3-diaryl propenones and their cyclized pyrimidine derivatives as tubulin polymerization inhibitors
Published in Results in Chemistry (01-12-2023)“…[Display omitted] •Sixteen new chalcones and their cyclized pyrimidine derivatives were synthesized.•The lipidated 4,6-diaryl pyrimidine-2-amine 19 exhibited…”
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Synthesis and CYP24A1 inhibitory activity of ( E)-2-(2-substituted benzylidene)- and 2-(2-substituted benzyl)-6-methoxy-tetralones
Published in European journal of medicinal chemistry (01-10-2010)“…A series of ( E)-2-(2-substituted benzylidene)- and 2-(2-substituted benzyl)-6-methoxy-tetralones were prepared, using an efficient synthetic scheme, and…”
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Synthesis and CYP24A1 inhibitory activity of N-(2-(1H-imidazol-1-yl)-2-phenylethyl)arylamides
Published in Bioorganic & medicinal chemistry (15-07-2010)“…A series of N-(2-(1H-imidazol-1-yl)-2-phenylethyl)arylamides were prepared and evaluated for their inhibitory activity against human cytochrome P450C24A1…”
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