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...
Fang, Yuanying Zhang, Shaokun Li, Min Xiong, Lijuan Tu, Liangxing Xie, Saisai Jin, Yi Liu, Yanhua Yang, Zunhua Liu, Ronghua
...
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...
Ali, M Barakat, Assem El-Faham, Ayman Al-Rasheed, Hessa H Dahlous, Kholoud Al-Majid, Abdullah Mohammed Sharma, Anamika Yousuf, Sammer Sanam, Mehar Ul-Haq, Zaheer
...
Published in
Journal of enzyme inhibition and medicinal chemistry
A new series of thiobarbituric (thiopyrimidine trione) enamine derivatives and its analogues barbituric acid derivatives was synthesised, characterised, and screen for in vitro evaluation of α-glucosidase enzyme inhibition and anti-glycation activity. This series of compounds were found to inhibit α-glucosidase activity in a reversible mixed-type m...
Pustenko, Aleksandrs Nocentini, Alessio Balašova, Anastasija Krasavin, Mikhail Žalubovskis, Raivis Supuran, Claudiu T
Published in
Journal of enzyme inhibition and medicinal chemistry
A series of 3H-1,2-benzoxathiepine 2,2-dioxides incorporating 7-acylamino moieties were obtained by an original procedure starting from 5-nitrosalicylaldehyde, which was treated with propenylsulfonyl chloride followed by Wittig reaction of the bis-olefin intermediate. The new derivatives, belonging to the homosulfocoumarin chemotype, were assayed a...
Song, Yoojin Park, Sun You Wu, Zhexue Liu, Kwang-Hyeon Seo, Young Ho
Published in
Journal of enzyme inhibition and medicinal chemistry
Chlorambucil is a nitrogen mustard-based DNA alkylating drug, which is widely used as a front-line treatment of chronic lymphocytic leukaemia (CLL). Despite its widespread application and success for the initial treatment of leukaemia, a majority of patients eventually develop acquired resistance to chlorambucil. In this regard, we have designed an...
Kim, Suwon Jo, Seri Kim, Mi-Sun Shin, Dong Hae
Published in
Journal of enzyme inhibition and medicinal chemistry
Frequent occurrences of multi-drug resistance of pathogenic Gram-negative bacteria threaten human beings. The CMP-2-keto-3-deoxy-d-manno-octulosonic acid biosynthesis pathway is one of the new targets for antibiotic design. 2-Keto-3-deoxy-d-manno-octulosonate cytidylyltransferase (KdsB) is the key enzyme in this pathway. KdsB proteins from Burkhold...
