Xiao-Bao Shen,Yang Wang,Xuan-Zhen Han et al.
Xiao-Bao Shen et al.
Basis on molecular docking and pharmacophore analysis of naphthoquinone moiety, a total of 23 compounds were designed and synthesised. With the help of reverse targets searching, anti-cancer activity was preliminarily evaluated, most of the...
Exploring the fatty acid amide hydrolase and cyclooxygenase inhibitory properties of novel amide derivatives of ibuprofen [0.03%]
探究新异丁苯胺衍生物的脂肪酰胺酶和环氧化酶抑制特性
Alessandro Deplano,Jessica Karlsson,Mona Svensson et al.
Alessandro Deplano et al.
Inhibition of fatty acid amide hydrolase (FAAH) reduces the gastrointestinal damage produced by non-steroidal anti-inflammatory agents such as sulindac and indomethacin in experimental animals, suggesting that a dual-action FAAH-cyclooxygen...
Unveiling the interaction profile of rosmarinic acid and its bioactive substructures with serum albumin [0.03%]
鼠李糖酸及其生物活性亚结构与血清白蛋白相互作用的研究
Christina Papaemmanouil,Maria V Chatziathanasiadou,Christos Chatzigiannis et al.
Christina Papaemmanouil et al.
Rosmarinic acid, a phytochemical compound, bears diverse pharmaceutical profile. It is composed by two building blocks: caffeic acid and a salvianic acid unit. The interaction profile, responsible for the delivery of rosmarinic acid and its...
S-substituted 2-mercaptoquinazolin-4(3H)-one and 4-ethylbenzensulfonamides act as potent and selective human carbonic anhydrase IX and XII inhibitors [0.03%]
S-取代的2-巯基喹唑啉-4(3H)-酮和对乙基苯磺酰胺是人碳酐酶IX和XII的有效抑制剂
Adel S El-Azab,Alaa A-M Abdel-Aziz,Silvia Bua et al.
Adel S El-Azab et al.
We evaluated the hCA (CA, EC 4.2.1.1) inhibitory activity of novel 4-(2-(2-substituted-thio-4-oxoquinazolin-3(4H)-yl)ethyl)benzenesulfonamides (compounds 2-20) towards the isoforms I, II, IX, and XII. hCA Isoforms were effectively inhibited...
Synthesis and biological evaluation of 3-arylbenzofuranone derivatives as potential anti-Alzheimer's disease agents [0.03%]
3-芳基苯并呋喃酮衍生物作为潜在抗阿尔茨海默病制剂的合成与生物学评价
Jie Yang,Yinling Yun,Yuhang Miao et al.
Jie Yang et al.
Multi-target drugs can better address the cascade of events involved in oxidative stress and the reduction in cholinergic transmission that occur in Alzheimer's disease than cholinesterase inhibitors alone. We synthesised a series of 3-aryl...
Synthesis, antitumor activity, and molecular docking study of 2-cyclopentyloxyanisole derivatives: mechanistic study of enzyme inhibition [0.03%]
2-环戊氧基茴香醚衍生物的合成、抗肿瘤活性及分子对接研究：酶抑制作用机制研究
Walaa M El-Husseiny,Magda A-A El-Sayed,Adel S El-Azab et al.
Walaa M El-Husseiny et al.
A series of 24 compounds was synthesised based on a 2-cyclopentyloxyanisole scaffold 3-14 and their in vitro antitumor activity was evaluated. Compounds 4a, 4b, 6b, 7b, 13, and 14 had the most potent antitumor activity (IC50 range: 5.13-17....
Antiproliferative chromone derivatives induce K562 cell death through endogenous and exogenous pathways [0.03%]
抗增殖香豆素衍生物通过内外凋亡途径诱导K562细胞死亡
Runwei Jiao,Fanxing Xu,Xiaofang Huang et al.
Runwei Jiao et al.
A series of furoxan derivatives of chromone were prepared. The antiproliferative activities were tested against five cancer cell lines HepG2, MCF-7, HCT-116, B16, and K562, and two normal human cell lines L-02 and PBMCs. Among them, compoun...
Histidine residues at the copper-binding site in human tyrosinase are essential for its catalytic activities [0.03%]
组氨酸残基对人酪氨酶的铜结合部位及其催化活性是必不可少的
Hyangsoon Noh,Sung Jun Lee,Hyun-Joo Jo et al.
Hyangsoon Noh et al.
Tyrosinase is a copper-binding enzyme involved in melanin biosynthesis. However, the detailed structure of human tyrosinase has not yet been solved, along with the identification of the key sites responsible for its catalytic activity. We u...
Discovery of novel ATAD2 bromodomain inhibitors that trigger apoptosis and autophagy in breast cells by structure-based virtual screening [0.03%]
基于结构的虚拟筛选发现新型ATAD2溴结构域抑制剂可触发乳腺细胞凋亡和自噬
Dahong Yao,Jin Zhang,Jinhui Wang et al.
Dahong Yao et al.
ATAD2 has been reported to play an important role in the processes of numerous cancers and validated to be a potential therapeutic target. This work is to discover potent ATAD2 inhibitors and elucidate the underlying mechanisms in breast ca...
Synthesis, biological evaluation and molecular modelling of 2,4-disubstituted-5-(6-alkylpyridin-2-yl)-1 H-imidazoles as ALK5 inhibitors [0.03%]
作为ALK5抑制剂的2,4-取代-5-(6-烷基吡啶-2-基)-1H-咪唑的合成、生物评价及分子建模研究
Myoung-Soon Park,Hyun-Ju Park,Young Jae An et al.
Myoung-Soon Park et al.
A series of 2,4-disubstituted-5-(6-alkylpyridin-2-yl)-1H-imidazoles, 7a-c, 11a-h, and 16a-h has been synthesised and evaluated for their ALK5 inhibitory activity in an enzyme assay and in a cell-based luciferase reporter assay. Incorporatio...