Mechanistic and biological characterisation of novel N5-substituted paullones targeting the biosynthesis of trypanothione in Leishmania [0.03%]
新型N5位取代的paullone衍生物抑制利什曼原虫二氢叶酸还原酶及噻四氨合成的机制和生物学研究
Andrea Medeiros,Diego Benítez,Ricarda S Korn et al.
Andrea Medeiros et al.
Trypanothione synthetase (TryS) produces N1,N8-bis(glutathionyl)spermidine (or trypanothione) at the expense of ATP. Trypanothione is a metabolite unique and essential for survival and drug-resistance of trypanosomatid parasites. In this st...
Synthesis and evaluation of a large library of nitroxoline derivatives as pancreatic cancer antiproliferative agents [0.03%]
合成并评估硝喹啉衍生物大型库作为抗胰腺癌增殖剂的效果
Serena Veschi,Simone Carradori,Laura De Lellis et al.
Serena Veschi et al.
Pancreatic cancer (PC) is one of the deadliest carcinomas and in most cases, which are diagnosed with locally advanced or metastatic disease, current therapeutic options are highly unsatisfactory. Based on the anti-proliferative effects sho...
A study of Rose Bengal against a 2-keto-3-deoxy-d- manno-octulosonate cytidylyltransferase as an antibiotic candidate [0.03%]
玫瑰花青与酮糖八碳吡喃糖酸基转移酶作为抗生素候选药物的研究
Suwon Kim,Seri Jo,Mi-Sun Kim et al.
Suwon Kim et al.
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...
Activation studies of the β-carbonic anhydrases from Escherichia coli with amino acids and amines [0.03%]
丙氨酸和胺活化大肠杆菌β-碳酸酐酶的研究
Alessio Nocentini,Sonia Del Prete,Margaret D Mastrolorenzo et al.
Alessio Nocentini et al.
A β-carbonic anhydrase (CA, EC 4.2.1.1) from the widespread bacterium Escherichia coli (EcoCAβ), encoded by the CynT2 gene, has been investigated for its catalytic properties and enzymatic activation by a panel of amino acids and amines. ...
Cinnamic acid derivatives: inhibitory activity against Escherichia coli β-glucuronidase and structure-activity relationships [0.03%]
肉桂酸衍生物对大肠杆菌β-葡萄糖醛酸酶的抑制活性及其构效关系研究
Xing-Nuo Li,Lu-Xia Hua,Tao-Shun Zhou et al.
Xing-Nuo Li et al.
Gut microbial β-glucuronidase (GUS) is a potential therapeutic target to reduce gastrointestinal toxicity caused by irinotecan. In this study, the inhibitory effects of 17 natural cinnamic acid derivatives on Escherichia coli GUS (EcGUS) w...
The effects of cardiac drugs on human erythrocyte carbonic anhydrase I and II isozymes [0.03%]
心脏药物对人红细胞碳酐酶同工酶I和II的影响研究
Onur Argan,Kübra Çıkrıkçı,Aybike Baltacı et al.
Onur Argan et al.
Cardiovascular diseases are the leading cause of mortality worldwide. In recent years, the relationship between carbonic anhydrase inhibitors and atherosclerosis has attracted attention. In this study, we aimed to determine the in vitro eff...
Topoisomerases inhibition and DNA binding mode of daunomycin-oligoarginine conjugate [0.03%]
dauromycin-寡精氨酸结合物的拓扑异构酶抑制和DNA结合作用研究
Valeria Visone,Ildikó Szabó,Giuseppe Perugino et al.
Valeria Visone et al.
Cancer is a major health issue adsorbing the attention of a biomedical research. To fight this disease, new drugs are developed, specifically tailored to target biological pathways or peculiar components of the tumour cells. Particularly in...
Huarui Zhang,Jun Lu,Jin Liu et al.
Huarui Zhang et al.
Exosomes are small membrane vesicles released by most eukaryotic cells. They are considered to play an essential role in cell-to-cell communication, and It is also found that they serve as functional mediators in many severe diseases, inclu...
Design, synthesis, and anticonvulsant effects evaluation of nonimidazole histamine H3 receptor antagonists/inverse agonists containing triazole moiety [0.03%]
三唑类非咪唑组胺H₃受体拮抗剂/反向激动剂的设计、合成及抗惊厥作用评价
Mingxia Song,Rui Yan,Yanhui Zhang et al.
Mingxia Song et al.
Histamine H3 receptors (H3R) antagonists/inverse agonists are becoming a promising therapeutic approach for epilepsy. In this article, novel nonimidazole H3R antagonists/inverse agonists have been designed and synthesised via hybriding the ...
Novel [(N-alkyl-3-indolylmethylene)hydrazono]oxindoles arrest cell cycle and induce cell apoptosis by inhibiting CDK2 and Bcl-2: synthesis, biological evaluation and in silico studies [0.03%]
新型[(N-烷基-3-吲哚亚甲基)肼基氧]奥氏异丁茋通过抑制CDK2和Bcl-2诱导细胞凋亡并阻滞细胞周期：合成、生物评价及计算机辅助研究
Tarfah Al-Warhi,Mahmoud F Abo-Ashour,Hadia Almahli et al.
Tarfah Al-Warhi et al.
As a continuation for our previous work, a novel set of N-alkylindole-isatin conjugates (7, 8a-c, 9 and 10a-e) is here designed and synthesised with the prime aim to develop more efficient isatin-based antitumor candidates. Utilising the SA...