Journal of Enzyme Inhibition and Medicinal Chemistry
Papers 2,733
1 page of 274 pages (2,733 results)
#1Loredana Salerno (University of Catania)H-Index: 26
#2Luca Vanella (University of Catania)H-Index: 40
Last. Sebastiano Intagliata (University of Catania)H-Index: 14
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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 ...
#1Guangcheng WangH-Index: 16
#2Meiyan FanH-Index: 4
Last. Zhiyun Peng (SHOU: 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 ...
#1Wagdy M. Eldehna (Kafrelsheikh University)H-Index: 26
#2Rofaida Salem (Kafrelsheikh University)H-Index: 1
Last. Hatem A. Abdel-AzizH-Index: 36
view all 11 authors...
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...
#1Ahmed M. Shawky (UQU: Umm al-Qura University)H-Index: 10
#2Nashwa A. Ibrahim (UQU: Umm al-Qura University)H-Index: 7
Last. Ahmed M. Gouda (UQU: Umm al-Qura University)H-Index: 12
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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...
#1Katarzyna Jakimiuk (Medical University of Białystok)H-Index: 3
#2Jakub Gesek (Medical University of Białystok)H-Index: 1
Last. Michał Tomczyk (Medical University of Białystok)H-Index: 20
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Elastase is a proteolytic enzyme belonging to the family of hydrolases produced by human neutrophils, monocytes, macrophages, and endothelial cells. Human neutrophil elastase is known to play multiple roles in the human body, but an increase in its activity may cause a variety of diseases. Elastase inhibitors may prevent the development of psoriasis, chronic kidney disease, respiratory disorders (including COVID-19), immune disorders, and even cancers. Among polyphenolic compounds, some flavonoi...
#1Xin Wang (NMU: Nanjing Medical University)
#2Xin Yang (NMU: Nanjing Medical University)H-Index: 1
Last. Jingyu Zhu (JU: Jiangnan University)
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Serine palmitoyltransferase (SPT) plays the key role on catalysing the formation of 3-ketodihydrosphingosine, which is the first step of the de novo biosynthesis of sphingolipids. SPT is linked to ...
#1Ana I. Ahuja-Casarín (BUAP: Benemérita Universidad Autónoma de Puebla)H-Index: 1
#2Penélope Merino-Montiel (BUAP: Benemérita Universidad Autónoma de Puebla)H-Index: 11
Last. José G. Fernández-Bolaños (University of Seville)H-Index: 21
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We have designed unprecedented cholinesterase inhibitors based on 1-deoxynojirimycin as potential anti-Alzheimer’s agents. Compounds are comprised of three key structural motifs: the iminosugar, fo...
#1Yang Li (CMU: China Medical University)H-Index: 3
#2Ying Sun (CMU: China Medical University)H-Index: 1
Last. Guojun Zhang (CMU: China Medical University)H-Index: 1
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Histone lysine specific demethylase 1 (LSD1) has emerged as an attractive molecule target for the discovery of potently anticancer drugs to treat leukaemia. In this study, a series of novel chalcon...
#1R Vinci (UCSC: Catholic University of the Sacred Heart)H-Index: 4
#2Daniela PedicinoH-Index: 16
Last. Giovanna Liuzzo (UCSC: Catholic University of the Sacred Heart)H-Index: 56
view all 11 authors...
Acute Coronary Syndromes (ACS) with plaque erosion display dysregulated hyaluronan metabolism, with increased hyaluronidase-2 (HYAL2) expression. However, the expression and the role of this enzyme on platelets has never been explored. We evaluated the platelet's HYAL2 (pltHYAL2) levels on I) stable angina (SA) and II) ACS patients, furtherly sub-grouped in Intact-Fibrous-Cap (IFC) and Ruptured-Fibrous-Cap (RFC), according to Optical Coherence Tomography. We assessed the HYAL2 role through an in...
#1Bhuwan Prasad Awasthi (YU: Yeungnam University)
#2Prakash Chaudhary (YU: Yeungnam University)H-Index: 2
Last. Byeong-Seon Jeong (YU: Yeungnam University)H-Index: 16
view all 6 authors...
Sorafenib is recommended as the primary therapeutic drug for patients with hepatocellular carcinoma. To discover a new compound that avoids low response rates and toxic side effects that occur in sorafenib therapy, we designed and synthesized new hybrid compounds of sorafenib and 2,4,5-trimethylpyridin-3-ols. Compound 6 was selected as the best of 24 hybrids that inhibit each of the four Raf kinases. The anti-proliferative activity of 6 in HepG2, Hep3B, and Huh7 cell lines was slightly lower tha...
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