Search Results - "Abdellatif, Khaled R A"
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Synthesis, EGFR Inhibition and Anti-cancer Activity of New 3,6-dimethyl-1-phenyl-4-(substituted-methoxy)pyrazolo[3,4-d] pyrimidine Derivatives
Published in Anti-cancer agents in medicinal chemistry (01-01-2017)“…as EGFR inhibitors, mammalian target of rapamycin (mTOR) inhibitors, Src or dual Src/Abl inhibitors, glycogen synthase kinase-3b (GSK-3b) inhibitors or cyclin…”
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2
Ethanesulfohydroxamic Acid Ester Prodrugs of Nonsteroidal Anti-inflammatory Drugs (NSAIDs): Synthesis, Nitric oxide and Nitroxyl Release, Cyclooxygenase Inhibition, Anti-inflammatory, and Ulcerogenicity Index Studies
Published in Journal of medicinal chemistry (10-03-2011)“…The carboxylic acid group of the anti-inflammatory (AI) drugs indo-methacin, (S)-naproxen and ibuprofen was covalently linked via a two-carbon ethyl spacer to…”
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3
Synthesis and biological evaluation of 2-(4-methylsulfonyl phenyl) indole derivatives: multi-target compounds with dual antimicrobial and anti-inflammatory activities
Published in BMC chemistry (30-03-2020)“…Three series of 2-(4-methylsulfonylphenyl) indole derivatives have been designed and synthesized. The synthesized compounds were assessed for their…”
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Synthesis and anti-inflammatory evaluation of new 1,3,5-triaryl-4,5-dihydro-1H-pyrazole derivatives possessing an aminosulphonyl pharmacophore
Published in Archives of pharmacal research (01-11-2015)“…A novel series of 2-pyrazoline derivatives 13a–l was synthesized via aldol condensation of 4-substituted acetophenones with appropriately substituted aldehydes…”
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5
Design, synthesis, modeling studies and biological evaluation of pyrazole derivatives linked to oxime and nitrate moieties as nitric oxide donor selective COX-2 and aromatase inhibitors with dual anti-inflammatory and anti-neoplastic activities
Published in Bioorganic chemistry (01-05-2023)“…[Display omitted] •Twelve pyrazole derivatives 10a-f and 11a-f were designed and synthesized.•10e-f and 11a-f showed good in vitro COX-2 selectivity.•10c, 11a…”
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Synthesis of Celecoxib Analogues Possessing a N-Difluoromethyl-1,2-dihydropyrid-2-one 5-Lipoxygenase Pharmacophore: Biological Evaluation as Dual Inhibitors of Cyclooxygenases and 5-Lipoxygenase with Anti-Inflammatory Activity
Published in Journal of medicinal chemistry (26-03-2009)“…A novel class of 1-(4-methanesulfonylphenyl and 4-aminosulfonylphenyl)-5-[4-(1-difluoromethyl-1,2-dihydropyrid-2-one)]-3-trifluoromethyl-1H-pyrazole hybrid…”
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7
Celecoxib prodrugs possessing a diazen-1-ium-1,2-diolate nitric oxide donor moiety: Synthesis, biological evaluation and nitric oxide release studies
Published in Bioorganic & medicinal chemistry letters (01-08-2010)“…A new class of anti-inflammatory (AI) cupferron prodrugs was synthesized wherein a diazen-1-ium-1,2-diolato ammonium salt, and its O2-methyl and…”
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8
Synthesis of new 4-[2-(4-methyl(amino)sulfonylphenyl)-5-trifluoromethyl-2 H-pyrazol-3-yl]-1,2,3,6-tetrahydropyridines: A search for novel nitric oxide donor anti-inflammatory agents
Published in Bioorganic & medicinal chemistry (01-10-2008)“…A group of 4-[2-(4-methyl(amino)sulfonylphenyl)-5-trifluoromethyl-2 H-pyrazol-3-yl]-1,2,3,6-tetrahydropyridines ( 11– 14) possessing a variety of substituents…”
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9
New 1,2,3-triazole/1,2,4-triazole hybrids linked to oxime moiety as nitric oxide donor selective COX-2, aromatase, B-RAFV600E and EGFR inhibitors celecoxib analogs: design, synthesis, anti-inflammatory/anti-proliferative activities, apoptosis and molecular modeling study
Published in Journal of enzyme inhibition and medicinal chemistry (01-12-2023)“…A new series of bis-triazole 19a-l was synthesised for the purpose of being hybrid molecules with both anti-inflammatory and anti-cancer activities and…”
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10
Synthesis and biological evaluation of N-difluoromethyl-1,2-dihydropyrid-2-one acetic acid regioisomers: Dual Inhibitors of cyclooxygenases and 5-lipoxygenase
Published in Bioorganic & medicinal chemistry letters (01-04-2010)“…A new group of acetic acid ( 7a– c, R 1 = H), and propionic acid ( 7d– f, R 1 = Me), regioisomers wherein a N-difluoromethyl-1,2-dihydropyrid-2-one moiety is…”
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11
New indomethacin analogs as selective COX‐2 inhibitors: Synthesis, COX‐1/2 inhibitory activity, anti‐inflammatory, ulcerogenicity, histopathological, and docking studies
Published in Archiv der Pharmazie (Weinheim) (01-04-2021)“…New indomethacin analogs 4a–g, 5, 6, 8a, and 8b were synthesized to overcome the nonselectivity and ulcer liability of indomethacin. All newly synthesized…”
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12
Synthesis and anticancer activity of some new pyrazolo[3,4-d]pyrimidin-4-one derivatives
Published in Molecules (Basel, Switzerland) (18-03-2014)“…3,6-Dimethyl-1-phenyl-1H-pyrazolo[3,4-d][1,3]oxazin-4-one (3) was prepared by hydrolysis of ethyl 5-amino-3-methyl-1-phenyl-1H-pyrazole-4-carboxylate (1) to…”
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Triaryl ( Z)-olefins suitable for radiolabeling with iodine-124 or fluorine-18 radionuclides for positron emission tomography imaging of estrogen positive breast tumors
Published in Bioorganic & medicinal chemistry letters (15-02-2011)“…A group of ( Z)-1,2-diphenyl-1-[4-[2-(4-methylpiperazin-1-yl)ethoxy]phenyl]but-1-enes were synthesized using methodologies that will allow incorporation of a […”
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14
Design, synthesis and biological screening of new 4-thiazolidinone derivatives with promising COX-2 selectivity, anti-inflammatory activity and gastric safety profile
Published in Bioorganic chemistry (01-02-2016)“…[Display omitted] •Two groups of thiazolidin-4-ones 4a–c and 8a–e were designed and synthesized.•Compounds 8c and 8d showed the best overall in vitro COX-2…”
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15
Synthesis, cyclooxygenase inhibition and anti-inflammatory evaluation of new 1,3,5-triaryl-4,5-dihydro-1H-pyrazole derivatives possessing methanesulphonyl pharmacophore
Published in Journal of enzyme inhibition and medicinal chemistry (01-12-2016)“…A new series of 1,3,5-triaryl-4,5-dihydro-1H-pyrazole derivatives 13a-p were synthesized via aldol condensation of 3/4-nitroacetophenones with appropriately…”
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16
Synthesis, cyclooxygenase inhibition, anti-inflammatory evaluation and ulcerogenic liability of new 1,5-diarylpyrazole derivatives
Published in Journal of enzyme inhibition and medicinal chemistry (03-11-2016)“…A new series of 1,5-diarylpyrazoles 10a-l was designed and synthesized for evaluation as COX inhibitors and as anti-inflammatory agents. All compounds were…”
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17
Synthesis of new 1-(4-methane(amino)sulfonylphenyl)-5-(4-substituted-aminomethylphenyl)-3-trifluoromethyl-1H-pyrazoles: A search for novel nitric oxide donor anti-inflammatory agents
Published in Bioorganic & medicinal chemistry letters (01-11-2014)“…[Display omitted] A group of 1-(4-methane(amino)sulfonylphenyl)-5-(4-substituted-aminomethylphenyl)-3-trifluoromethyl-1H-pyrazoles (12a–f) was synthesized and…”
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18
Celecoxib analogs possessing a N-(4-nitrooxybutyl)piperidin-4-yl or N-(4-nitrooxybutyl)-1,2,3,6-tetrahydropyridin-4-yl nitric oxide donor moiety: Synthesis, biological evaluation and nitric oxide release studies
Published in Bioorganic & medicinal chemistry letters (15-02-2010)“…A new group of hybrid nitric oxide (NO) releasing anti-inflammatory (AI) coxib prodrugs (NO-coxibs) wherein the para-tolyl moiety present in celecoxib was…”
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19
Synthesis and Biological Evaluation of New Diarylpyrazole and Triarylimidazoline Derivatives as Selective COX‐2 Inhibitors
Published in Archiv der Pharmazie (Weinheim) (01-08-2017)“…New series of diarylpyrazoles 8a–f and triarylimidazoline‐5‐ones 11a–g were synthesized and evaluated for their in vitro cyclooxygenase‐1 (COX‐1) and COX‐2…”
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20
Synthesis and biological evaluation of 1-(benzenesulfonamido)-2-[5-( N-hydroxypyridin-2(1 H)-one)]acetylene regioisomers: A novel class of 5-lipoxygenase inhibitors
Published in Bioorganic & medicinal chemistry (15-07-2008)“…A hitherto unknown class of linear acetylene regioisomers were designed such that a SO 2NH 2 group was located at the ortho-, meta-, or para-position of the…”
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