Search Results - "AWADALLAH, Fadi M"
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Design and synthesis of some new benzoylthioureido benzenesulfonamide derivatives and their analogues as carbonic anhydrase inhibitors
Published in Journal of enzyme inhibition and medicinal chemistry (01-12-2023)“…The present investigation reports the design and synthesis of three series of benzoylthioureido derivatives bearing either benzenesulfonamide 7a-f, benzoic…”
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Synthesis and anticancer activity of some 8-substituted-7-methoxy-2H-chromen-2-one derivatives toward hepatocellular carcinoma HepG2 cells
Published in European journal of medicinal chemistry (27-01-2015)“…Based on the reported anticancer activity of coumarin and pyrazoline derivatives, the present investigation dealt with the design and synthesis of coumarin…”
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Inhibition studies on a panel of human carbonic anhydrases with N1-substituted secondary sulfonamides incorporating thiazolinone or imidazolone-indole tails
Published in Journal of enzyme inhibition and medicinal chemistry (01-01-2018)“…Being the primary sulfonamide among the most efficient zinc binding group (ZBG) to design inhibitors for the metallo-enzymes carbonic anhydrases (CA, EC…”
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Design and synthesis of some new benzoylthioureido phenyl derivatives targeting carbonic anhydrase enzymes
Published in Journal of enzyme inhibition and medicinal chemistry (31-12-2022)“…The present study aimed to develop potent carbonic anhydrase inhibitors (CAIs). The design of the target compounds was based on modifying the structure of the…”
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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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Identification of new potent phthalazine derivatives with VEGFR-2 and EGFR kinase inhibitory activity
Published in European journal of medicinal chemistry (10-11-2016)“…Efforts to develop new antitumor agents are now directed towards multitarget therapies that are believed to have high potency and low tendency to resistance…”
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Sulfonamides as anticancer agents: A brief review on sulfonamide derivatives as inhibitors of various proteins overexpressed in cancer
Published in Bioorganic chemistry (01-06-2024)“…[Display omitted] Sulfonamides have gained prominence as versatile agents in cancer therapy, effectively targeting a spectrum of cancer-associated enzymes…”
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Synthesis and biological evaluation of novel coumarin–pyrazoline hybrids endowed with phenylsulfonyl moiety as antitumor agents
Published in European journal of medicinal chemistry (01-02-2013)“…Two groups of coumarin–pyrazoline hybrids were synthesized. The target compounds were obtained by cyclization of the coumarin chalcones with various…”
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Synthesis of some N-aroyl-2-oxindole benzenesulfonamide conjugates with carbonic anhydrase inhibitory activity
Published in Bioorganic chemistry (01-03-2020)“…[Display omitted] •Three series of benzenesulfonamide based compounds were prepared.•All compounds were screened for CA inhibition against CA I, II, IX and XII…”
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Design and synthesis of novel PARP-1 inhibitors based on pyridopyridazinone scaffold
Published in Bioorganic chemistry (01-06-2019)“…[Display omitted] •Twenty pyridopyridazinone were synthesized.•Target compounds were evaluated as PARP-1 enzyme inhibitors.•The best PARP-1 inhibition results…”
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Synthesis, carbonic anhydrase inhibition and cytotoxic activity of novel chromone-based sulfonamide derivatives
Published in European journal of medicinal chemistry (26-05-2015)“…Four series of sulfonamides incorporating chromone moieties were synthesized and assessed for their cytotoxic activity against MCF-7 and A-549 cell lines,…”
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New quinazolinone–pyrimidine hybrids: Synthesis, anti-inflammatory, and ulcerogenicity studies
Published in European journal of medicinal chemistry (01-07-2012)“…Two groups of hybrid compounds: the quinazolinone–dihydropyrimidines and quinazolinone–pyrimidines, were synthesized. The starting derivative 3 was reacted…”
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Molecular docking simulation, synthesis and 3D pharmacophore studies of novel 2-substituted-5-nitro-benzimidazole derivatives as anticancer agents targeting VEGFR-2 and c-Met
Published in Bioorganic chemistry (01-04-2018)“…3D QSAR based pharmacophore models of 12e in Fig. (a) non-small lung cancer and Fig.(b) colorectal cancer cell lines. IC50 = 2.19 ± 0.09 and 10.97 ± 0.09 µM,…”
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Synthesis of some dihydropyrimidine-based compounds bearing pyrazoline moiety and evaluation of their antiproliferative activity
Published in European journal of medicinal chemistry (2013)“…Two series of 2-(3,5-diaryl-4,5-dihydropyrazol-1-yl)-1-methyl-6-oxo-4-phenyl-1,6-dihydropyrimidine-5-carbonitriles 5a–h and…”
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Synthesis, vasorelaxant activity, and molecular modeling study of some new phthalazine derivatives
Published in European journal of medicinal chemistry (01-06-2012)“…New phthalazine-based vasodilators were synthesized through the chloroacylation of the starting compound 1-hydrazinophthalazine 4 to give the two key…”
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Design, synthesis and molecular modeling study for some new 2-substituted benzimidazoles as dual inhibitors for VEGFR-2 and c-Met
Published in Future medicinal chemistry (01-03-2018)“…Computer-aided drug design techniques were adopted to design three series of 2-substituted-5-nitrobenzimidazole derivatives hybridized with piperzine ,…”
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Design and synthesis of potent 1,2,4-trisubstituted imidazolinone derivatives with dual p38αMAPK and ERK1/2 inhibitory activity
Published in European journal of medicinal chemistry (13-04-2015)“…The synthesis of new 1,2,4-trisubstituted imidazolinone derivatives was described. The new compounds were designed as dual p38αMAPK and ERK1/2 inhibitors…”
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4-Substituted-1-phenyl-1H-pyrazolo[3,4-d]pyrimidine Derivatives: Design, Synthesis, Antitumor and EGFR Tyrosine Kinase Inhibitory Activity
Published in Chemical biology & drug design (01-05-2015)“…Four series of some 4‐substituted‐1‐phenyl‐1H‐pyrazolo[3,4‐d]pyrimidine derivatives 5a–f, 6a–f, 8a–f, and 9a–f were designed to be screened for their antitumor…”
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Novel substituted and fused pyrrolizine derivatives: Synthesis, anti-inflammatory and ulcerogenecity studies
Published in European journal of medicinal chemistry (01-02-2010)“…Synthesis of several substituted pyrrolizines 10a-f, 11a-f, 13a-c, pyrimidopyrrolizines 14a-c, 15a-c, and pyrrolizinopyrimidoisoindoles 12a-c was discussed…”
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