Search Results - "Osman, Essam Eldin A."
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Design and synthesis of some barbituric and 1,3-dimethylbarbituric acid derivatives: A non-classical scaffold for potential PARP1 inhibitors
Published in Bioorganic chemistry (01-11-2020)“…[Display omitted] •Barbituric acid derivatives were designed as non-classical PARP1 inhibitors.•The synthesized compounds revealed nanomolar inhibition against…”
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Synthesis and biological evaluation of novel xanthine derivatives as potential apoptotic antitumor agents
Published in European journal of medicinal chemistry (15-08-2019)“…A series of novel xanthine/NO donor hybrids containing 1,3,8-trisubstituted or 1,8-disubstituted xanthine derivatives were designed and synthesized. The…”
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Design and synthesis of novel cytotoxic fluoroquinolone analogs through topoisomerase inhibition, cell cycle arrest, and apoptosis
Published in Scientific reports (13-03-2023)“…To exploit the advantageous properties of approved drugs to hasten anticancer drug discovery, we designed and synthesized a series of fluoroquinolone (FQ)…”
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5-Chlorobenzofuran-2-carboxamides: From allosteric CB1 modulators to potential apoptotic antitumor agents
Published in European journal of medicinal chemistry (01-09-2019)“…Cannabinoids as THC and the CB1 allosteric modulator CBD were reported to have antiproliferative activities with no reports for other CB1 allosteric modulators…”
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“Turn-On” Quinoline-Based Fluorescent Probe for Selective Imaging of Tau Aggregates in Alzheimer’s Disease: Rational Design, Synthesis, and Molecular Docking
Published in ACS sensors (25-06-2021)“…Tau aggregation is believed to have a strong association with the level of cognitive deficits in Alzheimer’s disease (AD). Thus, optical brain imaging of tau…”
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Novel 3,6-Disubstituted Pyridazine Derivatives Targeting JNK1 Pathway: Scaffold Hopping and Hybridization-Based Design, Synthesis, Molecular Modeling, and In Vitro and In Vivo Anticancer Evaluation
Published in ACS omega (03-09-2024)“…A series of novel 3,6-disubstituted pyridazine derivatives were designed, synthesized, and biologically evaluated as preclinical anticancer candidates…”
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Ironing Out the Mechanism of gp130 Signaling
Published in Pharmacological reviews (16-10-2024)“…gp130 functions as a shared signal-transducing subunit not only for interleukin (IL)-6 but also for eight other human cytokine receptor complexes. The IL-6…”
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Design, synthesis and molecular docking of novel diarylcyclohexenone and diarylindazole derivatives as tubulin polymerization inhibitors
Published in Journal of enzyme inhibition and medicinal chemistry (01-01-2017)“…New target compounds were designed as inhibitors of tubulin polymerization relying on using two types of ring B models (cyclohexenone and indazole) to replace…”
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Why All the Fury over Furin?
Published in Journal of medicinal chemistry (24-02-2022)“…Analysis of the SARS-CoV-2 sequence revealed a multibasic furin cleavage site at the S1/S2 boundary of the spike protein distinguishing this virus from…”
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Design and Synthesis of Orally Active Quinolyl Pyrazinamides as Sigma 2 Receptor Ligands for the Treatment of Pancreatic Cancer
Published in Journal of medicinal chemistry (09-02-2023)“…Sigma 2 receptor (σ2R) is overexpressed in select cancers and is regarded as a biomarker for tumor proliferation. σ2R ligands are emerging as promising…”
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Analytical investigation of different mathematical approaches utilizing manipulation of ratio spectra
Published in Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy (05-01-2018)“…This work represents a comparative study of different approaches of manipulating ratio spectra, applied on a binary mixture of ciprofloxacin HCl and…”
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COVID-19: Living through Another Pandemic
Published in ACS infectious diseases (10-07-2020)“…Novel beta-coronavirus SARS-CoV-2 is the pathogenic agent responsible for coronavirus disease-2019 (COVID-19), a globally pandemic infectious disease. Due to…”
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Design and synthesis of novel furan, furo[2,3-d]pyrimidine and furo[3,2-e][1,2,4]triazolo[1,5-c]pyrimidine derivatives as potential VEGFR-2 inhibitors
Published in Bioorganic chemistry (01-11-2021)“…[Display omitted] •New furan, furopyrimidine and furotriazolopyrimidine derivatives were synthesized as potential VEGFR-2 inhibitors.•Furopyrimidine 8b and…”
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Design, synthesis and docking studies of novel benzopyrone derivatives as anticonvulsants
Published in Bioorganic chemistry (01-05-2020)“…[Display omitted] •Synthesis of novel benzopyrone derivatives as anticonvulsants.•In preliminary phase I screening, compound 6 exhibited the most potent Fig…”
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Novel pyrazolo[3,4-d]pyrimidines as dual Src-Abl inhibitors active against mutant form of Abl and the leukemia K-562 cell line
Published in European journal of medicinal chemistry (10-11-2016)“…Some novel 6-substituted pyrazolo[3,4-d]pyrimidines 4, 5, 6a-d, 7a-c, 8 and pyrazolo[4,3-e][1,2,4]triazolo[4,3-a]pyrimidines 9a-c, 10a-c, 11, 12a,b, 13a-c and…”
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Design, synthesis and biological evaluation of some novel quinazolinone derivatives as potent apoptotic inducers
Published in Future medicinal chemistry (01-05-2018)“…Novel quinazolinone and triazinoquinazolinone derivatives were designed and synthesized as apoptotic inducers. Most of the synthesized compounds showed…”
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Design and synthesis of novel 5-(4-chlorophenyl)furan derivatives with inhibitory activity on tubulin polymerization
Published in Future medicinal chemistry (01-08-2018)“…Discovery of novel series of colchicine binding site inhibitors (CBSIs). Isoxazoline , pyrazoline and , cyclohexenone and or pyridine derivatives were…”
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