Journal of Enzyme Inhibition and Medicinal Chemistry
Papers 2714
1 page of 272 pages (2,714 results)
Acetyl-CoA carboxylase (ACC) is a crucial enzyme in fatty acid metabolism, which plays a major role in the occurrence and development of certain tumours. Herein, one potential ACC inhibitor (6a) was identified through high-throughput virtual screening (HTVS), and a series of 4-phenoxy-phenyl isoxazoles were synthesised for structure-activity relationship (SAR) studies. Among these compounds, 6g exhibited the most potent ACC inhibitory activity (IC50=99.8 nM), which was comparable to that of CP-6...
#1Rosa Merlo (National Research Council)H-Index: 4
#2Diego CaprioglioH-Index: 10
Last. Giuseppe Perugino (National Research Council)H-Index: 20
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SNAP-tag ® is a powerful technology for the labelling of protein/enzymes by using benzyl-guanine (BG) derivatives as substrates. Although commercially available or ad hoc produced, their synthesis ...
1 CitationsSource
#1Hong-Yan Guo (Yanbian University)H-Index: 1
#2Zheng-Ai Chen (Yanbian University)H-Index: 1
Last. Zhe-Shan Quan (Yanbian University)H-Index: 24
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Nature products have been extensively used in the discovery and development of new drugs, as the most important source of drugs. The triazole ring is one of main pharmacophore of the nitrogen-containing heterocycles. Thus, a new class of triazole-containing natural product conjugates has been synthesised. These compounds reportedly exert anticancer, anti-inflammatory, antimicrobial, antiparasitic, antiviral, antioxidant, anti-Alzheimer, and enzyme inhibitory effects. This review summarises the r...
#1Guangcheng WangH-Index: 13
#2Meiyan FanH-Index: 1
Last. Zhiyun Peng (Shanghai Ocean University)H-Index: 4
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A new series of sulphonamide derivatives bearing naphthalene moiety were synthesised and evaluated for their antiproliferative and tubulin polymerisation inhibitory activities. These new compounds ...
#1Ahmed M. Shawky (UQU: Umm al-Qura University)H-Index: 9
#2Nashwa A. Ibrahim (UQU: Umm al-Qura University)H-Index: 5
Last. Ahmed M. Gouda (UQU: Umm al-Qura University)H-Index: 11
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In the current study, virtual screening of a small library of 1302 pyrrolizines bearing urea/thiourea moieties was performed. The top-scoring hits were synthesised and evaluated for their cytotoxic...
5 CitationsSource
#1Wagdy M. Eldehna (Kafrelsheikh University)H-Index: 25
#2Rofaida Salem (Kafrelsheikh University)H-Index: 1
Last. Hatem A. Abdel-AzizH-Index: 32
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In the current work, a new set of carbohydrazide linked benzofuran-isatin conjugates (5a-e and 7a-i) was designed and synthesised. The anticancer activity for compounds (5b-d, 7a, 7b, 7d and 7g) was measured against NCI-55 human cancer cell lines. Compound 5d was the most efficient, and thus subjected to the five-dose screen where it showed excellent broad activity against almost all tested cancer subpanels. Furthermore, all conjugates (5a-e and 7a-i) showed a good anti-proliferative activity to...
#1Loredana Salerno (University of Catania)H-Index: 25
#2Luca Vanella (University of Catania)H-Index: 37
Last. Sebastiano Intagliata (University of Catania)H-Index: 13
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In this work, the first mutual prodrug of 5-fluorouracil and heme oxygenase1 inhibitor (5-FU/HO-1 hybrid) has been designed, synthesised, and evaluated for its in vitro chemical and enzymatic hydrolysis stability. Predicted in silico physicochemical properties of the newly synthesised hybrid (3) demonstrated a drug-like profile with suitable Absorption, Distribution, Metabolism, and Excretion (ADME) properties and low toxic liabilities. Preliminary cytotoxicity evaluation towards human prostate ...
#1Tehreem Tahir (IUB: Islamia University)H-Index: 2
#2Mirza Imran Shahzad (IUB: Islamia University)H-Index: 1
Last. Mariusz MojzychH-Index: 12
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In the present study, a series of azo derivatives (TR-1 to TR-9) have been synthesised via the diazo-coupling approach between substituted aromatic amines with phenol or naphthol derivatives. The compounds were evaluated for their therapeutic applications against alpha-glucosidase (anti-diabetic) and pathogenic bacterial strains E. coli (gram-negative), S. aureus (gram-positive), S. aureus (gram-positive) drug-resistant strain, P. aeruginosa (gram-negative), P. aeruginosa (gram-negative) drug-re...
#1Daniel A. S. Kitagawa (IME: Instituto Militar de Engenharia)H-Index: 4
Last. Angelo A.T. da SilvaH-Index: 7
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Organophosphorus poisoning caused by some pesticides and nerve agents is a life-threating condition that must be swiftly addressed to avoid casualties. Despite the availability of medical countermeasures, the clinically available compounds lack a broad spectrum, are not effective towards all organophosphorus toxins, and have poor pharmacokinetics properties to allow them crossing the blood-brain barrier, hampering cholinesterase reactivation at the central nervous system. In this work, we design...
#1Tarek S. Ibrahim (KAU: King Abdulaziz University)H-Index: 9
#2Amr H. Moustafa (Sohag University)H-Index: 6
Last. Mamdouh F.A. Mohamed (Sohag University)H-Index: 10
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Two series of chalcone/aryl carboximidamide hybrids 4a–f and 6a–f were synthesised and evaluated for their inhibitory activity against iNOS and PGE2. The most potent derivatives were further checke...
Top fields of study
Organic chemistry
Carbonic anhydrase