Hybrid inhibitors of DNA and HDACs remarkably enhance cytotoxicity in leukaemia cells [0.03%]
兼具DNA和HDAC抑制作用的协同抑制剂在白血病细胞中显著增强细胞毒性
Yoojin Song,Sun You Park,Zhexue Wu et al.
Yoojin Song et al.
Chlorambucil is a nitrogen mustard-based DNA alkylating drug, which is widely used as a front-line treatment of chronic lymphocytic leukaemia (CLL). Despite its widespread application and success for the initial treatment of leukaemia, a ma...
Bacterial ι-carbonic anhydrase: a new active class of carbonic anhydrase identified in the genome of the Gram-negative bacterium Burkholderia territorii [0.03%]
芽孢杆菌ι-碳酸酐酶：芽孢菌territorii基因组中鉴定出的一种新的碳酸酐酶类型
Sonia Del Prete,Alessio Nocentini,Claudiu T Supuran et al.
Sonia Del Prete et al.
The carbonic anhydrases (CAs, EC 4.2.1.1) catalyse a simple but physiologically crucial reversible reaction, the carbon dioxide hydration with the production of bicarbonate and protons. In the last years, and especially, to the rapid emerge...
An overview on natural farnesyltransferase inhibitors for efficient cancer therapy [0.03%]
高效的癌症治疗用天然法尼基转移酶抑制剂研究综述
Xiaohan Dai,Yingni Sun,Ting Zhang et al.
Xiaohan Dai et al.
As one of the world's five terminally ills, tumours can cause important genetic dysfunction. However, some current medicines for tumours usually have strong toxic side effects and are prone to drug resistance. Studies have found that farnes...
Lipidomic analysis of cancer cells cultivated at acidic pH reveals phospholipid fatty acids remodelling associated with transcriptional reprogramming [0.03%]
酸性培养的癌细胞脂质组分析揭示与转录重构相关的磷脂脂肪酸改造
Lorena Urbanelli,Sandra Buratta,Mariantonia Logozzi et al.
Lorena Urbanelli et al.
Cancer cells need to modulate the biosynthesis of membrane lipids and fatty acids to adapt themselves to an accelerated rate of cell division and survive into an extracellular environment characterised by a low pH. To gain insight this cruc...
Inhibition of African swine fever virus protease by myricetin and myricitrin [0.03%]
杨梅素和杨梅皮素通过抑制非洲猪瘟病毒蛋白酶而具有抗非洲猪瘟病毒活性
Seri Jo,Suwon Kim,Dong Hae Shin et al.
Seri Jo et al.
African swine fever (ASF) caused by the ASF virus (ASFV) is the most hazardous swine disease. Since a huge number of pigs have been slaughtered to avoid a pandemic spread, intense studies on the disease should be followed quickly. Recent st...
Antiproliferative benzothiazoles incorporating a trimethoxyphenyl scaffold as novel colchicine site tubulin polymerisation inhibitors [0.03%]
一类新型夹竹桃麻科秋水仙碱聚合抑制剂的3,4,5-三甲氧基苯并噻唑类抗增殖化合物
Dong-Jun Fu,Si-Meng Liu,Fu-Hao Li et al.
Dong-Jun Fu et al.
Tubulin polymerisation inhibitors exhibited an important role in the treatment of patients with prostate cancer. Herein, we reported the medicinal chemistry efforts leading to a new series of benzothiazoles by a bioisosterism approach. Biol...
The antibiotic furagin and its derivatives are isoform-selective human carbonic anhydrase inhibitors [0.03%]
抗生素富拉吉因及其衍生物是异构体选择性的人类碳酸酐酶抑制剂
Aleksandrs Pustenko,Alessio Nocentini,Paola Gratteri et al.
Aleksandrs Pustenko et al.
The clinically used antibiotic Furagin and its derivatives possess inhibitory activity on human (h) carbonic anhydrases (CA, EC 4.2.1.1), some of which are highly expressed in various tissues and malignancies (hCA IX/XII). Furagin exhibited...
Preparation, carbonic anhydrase enzyme inhibition and antioxidant activity of novel 7-amino-3,4-dihydroquinolin-2(1H)-one derivatives incorporating mono or dipeptide moiety [0.03%]
含有单肽或双肽部分的新7-氨基-3,4-二氢喹啉-2（1H）-一氧化物衍生物的制备，碳酸酐酶酶抑制和抗氧化活性
Hasan Küçükbay,Zeynep Gönül,F Zehra Küçükbay et al.
Hasan Küçükbay et al.
New dipeptide-dihydroquinolinone derivatives were successfully synthesised by benzotriazole mediated nucleophilic acyl substitution reaction and their structures were elucidated by spectroscopic and analytic techniques. The carbonic anhydra...
1,2,4-Triazole-based anticonvulsant agents with additional ROS scavenging activity are effective in a model of pharmacoresistant epilepsy [0.03%]
一种有效的治疗难治性癫痫的三唑类抗惊厥化合物及其清除ROS的作用
Barbara Kaproń,Robert Czarnomysy,Mariusz Wysokiński et al.
Barbara Kaproń et al.
There are numerous studies supporting the contribution of oxidative stress to the pathogenesis of epilepsy. Prolonged oxidative stress is associated with the overexpression of ATP-binding cassette transporters, which results in antiepilepti...
6,7-Dimethoxy-2-phenethyl-1,2,3,4-tetrahydroisoquinoline amides and corresponding ester isosteres as multidrug resistance reversers [0.03%]
6,7-二甲氧基-2-(苯乙基)-1,2,3,4-四氢异喹啉酰胺及其相应的酯等价物作为逆转多药耐药的化合物
Laura Braconi,Gianluca Bartolucci,Marialessandra Contino et al.
Laura Braconi et al.
Aiming to deepen the structure-activity relationships of the two P-glycoprotein (P-gp) modulators elacridar and tariquidar, a new series of amide and ester derivatives carrying a 6,7-dimethoxy-2-phenethyl-1,2,3,4-tetrahydroisoquinoline scaf...