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Uracil as a Zn-Binding Bioisostere of the Allergic Benzenesulfonamide in the Design of Quinoline–Uracil Hybrids as Anticancer Carbonic Anhydrase Inhibitors
Faculty
Pharmacy
Year:
2022
Type of Publication:
ZU Hosted
Pages:
494
Authors:
Amany Mohamed Mohamed Elmahmoudy Sanger
Staff Zu Site
Abstract In Staff Site
Journal:
Pharmaceuticals mdpi
Volume:
15
Keywords :
Uracil , , Zn-Binding Bioisostere , , Allergic Benzenesulfonamide , , Design , Quinoline–Uracil Hybrids
Abstract:
A series of quinoline–uracil hybrids (10a–l) has been rationalized and synthesized. The inhibitory activity against hCA isoforms I, II, IX, and XII was explored. Compounds 10a–l demonstrated powerful inhibitory activity against all tested hCA isoforms. Compound 10h displayed the best selectivity profile with good activity. Compound 10d displayed the best activity profile with minimal selectivity. Compound 10l emerged as the best congener considering both activity (IC50 = 140 and 190 nM for hCA IX and hCA XII, respectively) and selectivity (S.I. = 13.20 and 9.75 for II/IX, and II/XII, respectively). The most active hybrids were assayed for antiproliferative and pro-apoptotic activities against MCF-7 and A549. In silico studies, molecular docking, physicochemical parameters, and ADMET analysis were performed to explain the acquired CA inhibitory action of all hybrids. A study of the structure–activity relationship revealed that bulky substituents at uracil N-1 were unfavored for activity while substituted quinoline and thiouracil were effective for selectivity
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Amany Mohamed Mohamed Elmahmoudy Sanger, "Novel Benzyloxyphenyl Pyrimidine-5-Carbonitrile Derivatives as Potential Apoptotic Antiproliferative Agents", Bentham Science Publishers, 2022
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Amany Mohamed Mohamed Elmahmoudy Sanger, "DOCKING, SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL PYRAZOLINE DERIVATIVES AS POTENTIAL ANTIMICROBIAL AND ANTITUMOR AGENTS", www.wjpr.net, 2016
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Amany Mohamed Mohamed Elmahmoudy Sanger, "SYNTHESIS OF NOVEL PYRIMIDINE AND FUSED PYRIMIDINE DERIVATIVES AND THEIR IN VITRO ANTIMICROBIAL AND CYTOTOXIC EVALUATION", www.wjpr.net, 2017
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Amany Mohamed Mohamed Elmahmoudy Sanger, "Synthesis, cytotoxic and antimicrobial activity of some new 3,4,5-trimethoxybenzyl-1,2,4- triazines and their condensed derivatives", www.cbijournal.com, 2011
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Department Related Publications
Etedaal Hassan Mohamed Abdulaal, "18. In situ annelation of enaminones by reaction with methyleneiminium intermediates", لايوجد, 1900
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Hanan Abdelraziek Abdelfattah Ali Hamied, "synthesis of some new imidazolones of expected antimicrobial activity", لايوجد, 1900
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Azza Mohamed Kadry , "35. Synthesis and potentiometric study of some dioxadiaza ionophores in ion selective electrodes", لايوجد, 1900
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Azza Mohamed Kadry , "16. Chemistry of quinazolines: Reinvestigation of the action of hydrazine on thioxo derivatives", لايوجد, 1900
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Azza Mohamed Kadry , "2. Reaction and rearrangement of 2,4-quinazolinediones", لايوجد, 1900
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