Li, Yang Sun, Ying Zhou, Yang Li, Xinyang Zhang, Huan Zhang, Guojun
Published in
Journal of enzyme inhibition and medicinal chemistry
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 chalcone derivatives were designed, synthesised and evaluated for their inhibitory activities against LSD1 in vitro. Among all these compounds, D6 displayed the...
Cornejo, Alberto Caballero, Julio Simirgiotis, Mario Torres, Vanessa Sánchez, Luisa Díaz, Nicolás Guimaraes, Marcela Hernández, Marcos Areche, Carlos Alfaro, Sergio
...
Published in
Journal of enzyme inhibition and medicinal chemistry
Parkinson's disease (PD) is a neurodegenerative disorder that affects adult people whose treatment is palliative. Thus, we decided to test three dammarane triterpenes 1, 1a, 1b, and we determined that 1 and 1a inhibit β-aggregation through thioflavine T rather than 1b. Since compound 1 was most active, we determined the interaction between α-synucl...
Ahmed, Marwa F Santali, Eman Y El-Haggar, Radwan
Published in
Journal of enzyme inhibition and medicinal chemistry
New piperazine-chalcone hybrids and related pyrazoline derivatives have been designed and synthesised as potential vascular endothelial growth factor receptor-2 (VEGFR-2) inhibitors. The National Cancer Institute (NCI) has selected six compounds to evaluate their antiproliferative activity in vitro against 60 human cancer cells lines. Preliminary s...
Ahuja-Casarín, Ana I Merino-Montiel, Penélope Vega-Baez, José Luis Montiel-Smith, Sara Fernandes, Miguel X Lagunes, Irene Maya, Inés Padrón, José M López, Óscar Fernández-Bolaños, José G
...
Published in
Journal of enzyme inhibition and medicinal chemistry
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, for interaction with cholinesterase catalytic anionic site (CAS); a hydrocarbon tether with variable lengths, and a fragment derived from 2-phenylethanol f...
Chao, Min-Wu Lin, Tony Eight HuangFu, Wei-Chun Chang, Chao-Di Tu, Huang-Ju Chen, Liang-Chieh Yen, Shih-Chung Sung, Tzu-Ying Huang, Wei-Jan Yang, Chia-Ron
...
Published in
Journal of enzyme inhibition and medicinal chemistry
The STE20 kinase family is a complex signalling cascade that regulates cytoskeletal organisation and modulates the stress response. This signalling cascade includes various kinase mediators, such as TAOK1 and MAP4K5. The dysregulation of the STE20 kinase pathway is linked with cancer malignancy. A small-molecule inhibitor targeting the STE20 kinase...
Hermanowicz, Justyna Magdalena Szymanowska, Anna Sieklucka, Beata Czarnomysy, Robert Pawlak, Krystyna Bielawska, Anna Bielawski, Krzysztof Kalafut, Joanna Przybyszewska, Alicja Surazynski, Arkadiusz
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Published in
Journal of Enzyme Inhibition and Medicinal Chemistry
Colorectal cancer (CRC) is the third leading cause of cancer-related deaths in men and in women. The impact of the new pyrazolo[4,3- e ]tetrazolo[1,5- b ][1,2,4]triazine sulphonamide ( MM-129 ) was evaluated against human colon cancer in vitro and in zebrafish xenografts. Our results show that this new synthesised compound effectively inhibits cell...
Floris, Sonia Fais, Antonella Medda, Rosaria Pintus, Francesca Piras, Alessandra Kumar, Amit Kuś, Piotr Marek Westermark, Gunilla Torstensdotter Era, Benedetta
Published in
Journal of Enzyme Inhibition and Medicinal Chemistry
Washingtonia filifera seeds have revealed to possess antioxidant properties, butyrylcholinesterase and xanthine oxidase inhibition activities. The literature has indicated a relationship between Alzheimer’s disease (AD) and type-2 diabetes (T2D). Keeping this in mind, we have now evaluated the inhibitory properties of W. filifera seed extracts on α...
Liu, Hongbo Ye, Fei Sun, Qi Liang, Hao Li, Chunmei Li, Siyang Lu, Roujian Huang, Baoying Tan, Wenjie Lai, Luhua
...
Published in
Journal of Enzyme Inhibition and Medicinal Chemistry
COVID-19 has become a global pandemic and there is an urgent call for developing drugs against the virus (SARS-CoV-2). The 3C-like protease (3CLpro) of SARS-CoV-2 is a preferred target for broad spectrum anti-coronavirus drug discovery. We studied the anti-SARS-CoV-2 activity of S. baicalensis and its ingredients. We found that the ethanol extract ...
David, Benoit Schneider, Pascal Schäfer, Philipp Pietruszka, Jörg Gohlke, Holger
Published in
Journal of Enzyme Inhibition and Medicinal Chemistry
For more than two decades, the development of potent acetylcholinesterase (AChE) inhibitors has been an ongoing task to treat dementia associated with Alzheimer’s disease and improve the pharmacokinetic properties of existing drugs. In the present study, we used three docking-based virtual screening approaches to screen both ZINC15 and MolPort data...
Bonardi, Alessandro Nocentini, Alessio Osman, Sameh Mohamed Alasmary, Fatmah Ali Almutairi, Tahani Mazyad Abdullah, Dalal Saied Gratteri, Paola Supuran, Claudiu T.
Published in
Journal of Enzyme Inhibition and Medicinal Chemistry
The binding mode of aromatic sulphonamides and clinically licenced drugs to the three carbonic anhydrase (CA, EC 4.2.1.1) isoforms from the human pathogen V. cholerae was here thouroghly characterised by a joint docking and molecular dynamics in silico protocol. In fact, VchCA, VchCAβ, and VchCAγ are crucial in the pathogen life cycle and growth an...
