Bioorganometallic derivatives of 4-hydrazino-benzenesulphonamide as carbonic anhydrase inhibitors: synthesis, characterisation and biological evaluation [0.03%]
4-叠氮基苯磺酰胺生物有机金属衍生物作为碳酸酐酶抑制剂：合成，表征及生物学评价
Jeremie Brichet,Rodrigo Arancibia,Emanuela Berrino et al.
Jeremie Brichet et al.
A series of bio-organometallic-hydrazones of the general formula [{(η5-C5H4)-C(R)=N-N(H)-C6H4-4-SO2NH2}]MLn(MLn = Re(CO)3, Mn(CO)3, FeCp; R=H, CH3) were prepared by reaction of formyl/acetyl organometallic precursors with 4-hydrazino-benze...
Synthesis, anti-inflammatory, cytotoxic, and COX-1/2 inhibitory activities of cyclic imides bearing 3-benzenesulfonamide, oxime, and β-phenylalanine scaffolds: a molecular docking study [0.03%]
含3-苯磺酰胺、肟和β-苯甘氨酸骨架环状亚胺的合成及其抗炎、细胞毒性及COX-1/2抑制活性：分子对接研究
Alaa A-M Abdel-Aziz,Adel S El-Azab,Nawaf A AlSaif et al.
Alaa A-M Abdel-Aziz et al.
Cyclic imides containing 3-benzenesulfonamide, oxime, and β-phenylalanine derivatives were synthesised and evaluated to elucidate their in vivo anti-inflammatory and ulcerogenic activity and in vitro cytotoxic effects. Most active anti-inf...
Exploring structure-activity relationship of S-substituted 2-mercaptoquinazolin-4(3H)-one including 4-ethylbenzenesulfonamides as human carbonic anhydrase inhibitors [0.03%]
含4-乙基苯磺酰胺的S取代的2-巯基喹唑啉-4（3H）-酮的人类碳酸酐酶抑制剂及其构效关系研究
Adel S El-Azab,Alaa A-M Abdel-Aziz,Hany E A Ahmed et al.
Adel S El-Azab et al.
Inhibitory action of newly synthesised 4-(2-(2-substituted-thio-4-oxoquinazolin-3(4H)-yl)ethyl)benzenesulfonamides compounds 2-13 against human carbonic anhydrase (CA, EC 4.2.1.1) (hCA) isoforms I, II, IX, and XII, was evaluated. hCA I was ...
Selective inhibitors for JNK signalling: a potential targeted therapy in cancer [0.03%]
选择性JNK信号通路抑制剂：癌症治疗的潜在靶向疗法
Qinghua Wu,Wenda Wu,Vesna Jacevic et al.
Qinghua Wu et al.
c-Jun N-terminal kinase (JNK) signalling regulates both cancer cell apoptosis and survival. Emerging evidence show that JNK promoted tumour progression is involved in various cancers, that include human pancreatic-, lung-, and breast cancer...
C-2 phenyl replacements to obtain potent quinoline-based Staphylococcus aureus NorA inhibitors [0.03%]
基于喹啉类耐甲氧西林金黄色葡萄球菌NorA抑制剂的C-2苯环衍生物替换研究
Tommaso Felicetti,Gianmarco Mangiaterra,Rolando Cannalire et al.
Tommaso Felicetti et al.
NorA is the most studied efflux pump of Staphylococcus aureus and is responsible for high level resistance towards fluoroquinolone drugs. Although along the years many NorA efflux pump inhibitors (EPIs) have been reported, poor information ...
Design, synthesis and α-glucosidase inhibition study of novel embelin derivatives [0.03%]
新型Embelin衍生物的设计、合成及α-葡萄糖苷酶抑制作用研究
Xiaole Chen,Min Gao,Rongchao Jian et al.
Xiaole Chen et al.
Embelin is a naturally occurring para-benzoquinone isolated from Embelia ribes (Burm. f.) of the Myrsinaceae family. It was first discovered to have potent inhibitory activity (IC50 = 4.2 μM) against α-glucosidase in this study. Then, fou...
Rakia Abd Alhameed,Emanuela Berrino,Zainab Almarhoon et al.
Rakia Abd Alhameed et al.
A small series of 2,4-dioxothiazolidinyl acetic acids was prepared from thiourea, chloroacetic acid, aromatic aldehydes, and ethyl-2-bromoacetate. They were assayed for the inhibition of four physiologically relevant carbonic anhydrase (CA,...
Design, synthesis and in vitro biological evaluation of quinazolinone derivatives as EGFR inhibitors for antitumor treatment [0.03%]
作为抗肿瘤药物的表皮生长因子受体抑制剂喹唑啉衍生物的设计、合成及体外生物学评价研究
Yi Le,Yiyuan Gan,Yihong Fu et al.
Yi Le et al.
In this paper, a series of novel 3-methyl-quinazolinone derivatives was designed, synthesised and evaluated for antitumor activity in vitro on wild type epidermal growth factor receptor tyrosine kinase (EGFRwt-TK) and three human cancer cel...
Coumarins from Magydaris pastinacea as inhibitors of the tumour-associated carbonic anhydrases IX and XII: isolation, biological studies and in silico evaluation [0.03%]
Magydaris过去因亚cea_pastinacea中的香豆素作为肿瘤相关碳酸酐酶IX和XII抑制剂：分离，生物研究及计算机辅助评估
Benedetta Fois,Simona Distinto,Rita Meleddu et al.
Benedetta Fois et al.
In an in vitro screening for human carbonic anhydrase (hCA) inhibiting agents from higher plants, the petroleum ether and ethyl acetate extracts of Magydaris pastinacea seeds selectively inhibited hCA IX and hCA XII isoforms. The phytochemi...
Effect of 6-Benzoyl-benzothiazol-2-one scaffold on the pharmacological profile of α-alkoxyphenylpropionic acid derived PPAR agonists [0.03%]
基于α-烷氧基苯基丙酸类PPAR激动剂的药物代谢动力学及药效活性的影响研究
Aurélie Hurtevent,Morgan Le Naour,Veronique Leclerc et al.
Aurélie Hurtevent et al.
A series of nitrogen heterocycles containing α-ethoxyphenylpropionic acid derivatives were designed as dual PPARα/γ agonist ligands for the treatment of type 2 diabetes (T2D) and its complications. 6-Benzoyl-benzothiazol-2-one was the mo...