Synthesis, characterisation, biological evaluation and in silico studies of sulphonamide Schiff bases [0.03%]
磺胺舒夫碱的合成、表征、生物评价及计算机辅助药物设计研究
Mustafa Durgun,Cüneyt Türkeş,Mesut Işık et al.
Mustafa Durgun et al.
Sulphonamides are biologically important compounds with low toxicity, many bioactivities and cost-effectiveness. Eight sulphonamide derivatives were synthesised and characterised by FT-IR, 13C NMR, 1H NMR, LC-MS and elemental analysis. Thei...
Imidazopyridine-fused [1,3]diazepinones: modulations of positions 2 to 4 and their impacts on the anti-melanoma activity [0.03%]
咪唑并吡啶稠合[1,3]二氮杂环辛酮：2-4位点修饰对抗黑色素瘤活性的影响
Paul Le Baccon-Sollier,Yohan Malki,Morgane Maye et al.
Paul Le Baccon-Sollier et al.
A series of 19 novel pyrido-imidazodiazepinones, with modulations of positions 2, 3 and 4 of the diazepine ring were synthesised and screened for their in vitro cytotoxic activities against two melanoma cell lines (A375 and MDA-MB-435) and ...
Novel sulindac derivatives: synthesis, characterisation, evaluation of antioxidant, analgesic, anti-inflammatory, ulcerogenic and COX-2 inhibition activity [0.03%]
新型舒林酸衍生物的合成、表征及抗氧化、镇痛、抗炎、胃毒性及COX-2抑制活性评价
Mashooq A Bhat,Mohamed A Al-Omar,Nawaf A Alsaif et al.
Mashooq A Bhat et al.
A new series of N'-(substituted phenyl)-2-(1-(4-(methylsulfinyl) benzylidene)-5-fluoro-2-methyl-1H-inden-3-yl) acetohydrazide derivatives (1 - 25) were prepared in good yields in an efficient manner. All the compounds were fully characteris...
The selenium-containing drug ebselen potently disrupts LEDGF/p75-HIV-1 integrase interaction by targeting LEDGF/p75 [0.03%]
含硒药物ebselen通过靶向LEDGF/p75干扰LEDGF/p75与HIV-1整合酶的相互作用
Da-Wei Zhang,Hao-Li Yan,Xiao-Shuang Xu et al.
Da-Wei Zhang et al.
Lens-epithelium-derived growth-factor (LEDGF/p75)-binding site on HIV-1 integrase (IN), is an attractive target for antiviral chemotherapy. Small-molecule compounds binding to this site are referred as LEDGF-IN inhibitors (LEDGINs). In this...
Use of an immobilised thermostable α-CA (SspCA) for enhancing the metabolic efficiency of the freshwater green microalga Chlorella sorokiniana [0.03%]
一种固定化热稳定性α-碳酸酐酶（SspCA）用于增强淡水绿微藻Chlorella sorokiniana代谢效率的应用研究
Giovanna Salbitani,Sonia Del Prete,Francesco Bolinesi et al.
Giovanna Salbitani et al.
There is significant interest in increasing the microalgal efficiency for producing high-quality products that are commonly used as food additives in nutraceuticals. Some natural substances that can be extracted from algae include lipids, c...
Synthesis and biological evaluation of (3/4-(pyrimidin-2-ylamino)benzoyl)-based hydrazine-1-carboxamide/carbothioamide derivatives as novel RXRα antagonists [0.03%]
一类新型RXRα拮抗剂(3/4-(嘧啶-2-氨基)苯甲酰基)肼类衍生物的设计、合成及活性研究
Jingbo Qin,Jie Liu,Chunxiao Wu et al.
Jingbo Qin et al.
Abnormal alterations in the expression and biological function of retinoid X receptor alpha (RXRα) have a key role in the development of cancer. Potential modulators of RXRα as anticancer agents are explored in growing numbers of studies....
Strong inhibitory activities and action modes of lipopeptides on lipase [0.03%]
脂肽类化合物对脂肪酶的强抑制作用及抑酶机制研究
Mei-Chun Chen,Tian-Tian Liu,Jie-Ping Wang et al.
Mei-Chun Chen et al.
Lipopeptides have been reported to exhibit anti-obesity effects. In this study, we obtained a Bacillus velezensis strain FJAT-52631 that could coproduce iturins, fengycins, and surfactins. Results showed that the FJAT-52631 crude lipopeptid...
Design, synthesis, molecular modelling and biological evaluation of novel 3-(2-naphthyl)-1-phenyl-1H-pyrazole derivatives as potent antioxidants and 15-Lipoxygenase inhibitors [0.03%]
一类新型的具有较强抗氧化及15-脂氧合酶抑制活性的3-(2-萘基)-1-苯基-1H-吡唑衍生物的设计合成、分子模拟与构效关系研究
Sahar A Ali,Samir Mohamed Awad,Ahmed Mohammed Said et al.
Sahar A Ali et al.
Oxidative stress is one of the main causes of significant severe diseases. The discovery of new potent antioxidants with high efficiency and low toxicity is a great demand in the field of medicinal chemistry. Herein, we report the design, s...
Activation studies of the β-carbonic anhydrases from Malassezia restricta with amines and amino acids [0.03%]
胺和氨基酸活化马拉色菌限制种的β-碳酐酶的研究
Andrea Angeli,Sonia Del Prete,Cynthia Ghobril et al.
Andrea Angeli et al.
The β-carbonic anhydrase (CA, EC 4.2.1.1) from the genome of the opportunistic pathogen Malassezia restricta (MreCA), which was recently cloned and characterised, herein has been investigated for enzymatic activation by a panel of amines a...
Antitumor properties of certain spirooxindoles towards hepatocellular carcinoma endowed with antioxidant activity [0.03%]
某些螺氧吲哚类化合物的抗肝癌及抗氧化活性研究
Sara T Al-Rashood,Ahmed R Hamed,Ghada S Hassan et al.
Sara T Al-Rashood et al.
In the current medical era, spirooxindole motif stands out as a privileged heterospirocyclic scaffold that represents the core for a wide range of bioactive naturally isolated products (such as Strychnofoline and spirotryprostatins A and B)...