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...
Kim, Suwon Jo, Seri Kim, Mi-Sun Shin, Dong Hae
Published in
Journal of enzyme inhibition and medicinal chemistry
d-Glycero-β-d-manno-heptose-1-phosphate adenylyltransferase from Burkholderia pseudomallei (BpHldC) is the fourth enzyme in the ADP-l-glycero-β-d-manno-heptose biosynthesis pathway producing a lipopolysaccharide core. Therefore, BpHldC is an anti-melioidosis target. Three ChemBridge compounds purchased from ChemBridge Corporation (San Diego, CA) we...
Cornejo, Alberto Caballero, Julio Simirgiotis, Mario Torres, Vanessa Sánchez, Luisa Díaz, Nicolás Guimaraes, Marcela Hernández, Marcos Areche, Carlos Alfaro, Sergio
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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...
Vinci, Ramona Pedicino, Daniela D'Aiello, Alessia Ciampi, Pellegrino Ponzo, Myriana Bonanni, Alice Russo, Giulio Montone, Rocco Antonio Massetti, Massimo Crea, Filippo
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Published in
Journal of enzyme inhibition and medicinal chemistry
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-g...
Zhang, Yuanyuan Xie, Chuan Liu, Yang Shang, Feng Shao, Rushiya Yu, Jing Wu, Chunxia Yao, Xinghui Liu, Dongfang Wang, Zhouyu
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Published in
Journal of enzyme inhibition and medicinal chemistry
Antibiotics resistance is becoming increasingly common, involving almost all antibiotics on the market. Diseases caused by drug resistant bacteria, such as MRSA, have high mortality and negatively affect public health. The development of new drugs would be an effective means of solving this problem. Modifications based on bioactive natural products...
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
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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
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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...
Zhang, Junmin Zheng, Zai-Qin Xu, Qianhe Li, Ya Gao, Kun Fang, Jianguo
Published in
Journal of enzyme inhibition and medicinal chemistry
Isolation and identification of natural products from plants is an essential approach for discovering drug candidates. Herein we report the characterization of three sesquiterpene lactones from a new genus Shangwua, e.g. onopordopicrin (ONP), C2, and C3, and evaluation of their pharmacological functions in interfering cellular redox signaling. Comp...
Fang, Yuanying Zhang, Shaokun Li, Min Xiong, Lijuan Tu, Liangxing Xie, Saisai Jin, Yi Liu, Yanhua Yang, Zunhua Liu, Ronghua
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Published in
Journal of enzyme inhibition and medicinal chemistry
GPR119 is a promising target for discovery of anti-type 2 diabetes mellitus agents. We described the optimisation of a novel series of pyrimido[5,4-b][1,4]oxazine derivatives as GPR119 agonists. Most designed compounds exhibited good agonistic activities. Among them, compound 10 and 15 demonstrated the potent EC50 values (13 and 12 nM, respectively...
