2-Thiopyrimidine/chalcone hybrids: design, synthesis, ADMET prediction, and anticancer evaluation as STAT3/STAT5a inhibitors [0.03%]
二噻嘧啶/查尔康因衍生物作为STAT3/STAT5A抑制剂的合成、设计及抗肿瘤活性评价
Phoebe F Lamie,John N Philoppes
Phoebe F Lamie
A novel 2-thiopyrimidine/chalcone hybrid was designed, synthesised, and evaluated for their cytotoxic activities against three different cell lines, K-562, MCF-7, and HT-29. The most active cytotoxic derivatives were 9d, 9f, 9n, and 9p (IC5...
Mario Cappiello,Francesco Balestri,Roberta Moschini et al.
Mario Cappiello et al.
The ability to catalyse a reaction acting on different substrates, known as "broad-specificity" or "multi-specificity", and to catalyse different reactions at the same active site ("promiscuity") are common features among the enzymes. These...
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...