Pyrrolo[2,1-f][1,2,4]triazine: a promising fused heterocycle to target kinases in cancer therapy [0.03%]
吡咯并[2,1-f][1,2,4]三嗪：一种有望用于癌症治疗激酶靶点的稠杂环化合物
Sarbjit Singh,Divya Utreja,Vimal Kumar
Sarbjit Singh
Cancer is the second leading cause of death worldwide responsible for about 10 million deaths per year. To date several approaches have been developed to treat this deadly disease including surgery, chemotherapy, radiation therapy, hormonal...
Dual monoamine oxidase B and acetylcholine esterase inhibitors for treating movement and cognition deficits in a C. elegans model of Parkinson's disease [0.03%]
在蠕虫模型中使用双重单胺氧化酶B和乙酰胆碱酯酶抑制剂治疗帕金森病的运动及认知缺陷
Jacob Boos,Ahmed Shubbar,Werner J Geldenhuys
Jacob Boos
Parkinson's disease (PD) is an age-associated neurodegenerative movement disorder that leads to loss of dopaminergic neurons and motor deficits. Approaches to neuroprotection and symptom management in PD include use of monoamine oxidase B (...
Synthesis and potential antimicrobial activity of novel α-aminophosphonates derivatives bearing substituted quinoline or quinolone and thiazole moieties [0.03%]
新型含取代喹啉或喹唑酮和噻唑基团的α-氨基磷酰衍生物的合成及其潜在抗菌活性研究
Bilal Litim,Abdelghani Djahoudi,Saida Meliani et al.
Bilal Litim et al.
To develop novel antimicrobial agents, and based on the biologically active heterocyclic quinoline and thiazole substituted, a series of novel α-aminophosphonates (9a-h) and (10i-l) derivatives that incorporated quinoline or quinolone, and...
Bio-evaluation of fluoro and trifluoromethyl-substituted salicylanilides against multidrug-resistant S. aureus [0.03%]
氟和三氟甲基水杨酰胺类化合物对多重耐药金黄色葡萄球菌的生物活性评价
Jhajan Lal,Grace Kaul,Abdul Akhir et al.
Jhajan Lal et al.
Methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Staphylococcus aureus (VRSA) are primary causes of skin and soft tissue infections worldwide. To address the emergency caused due to increasing multidrug-resistant ...
Innovation in the discovery of the HIV-1 attachment inhibitor temsavir and its phosphonooxymethyl prodrug fostemsavir [0.03%]
HIV-1附着抑制剂temsavir及其磷氧甲基前药fostemsavir的创新发现
Tao Wang,John F Kadow,Nicholas A Meanwell
Tao Wang
The discovery and development of fostemsavir (2), the tromethamine salt of the phosphonooxymethyl prodrug of temsavir (1), encountered significant challenges at many points in the preclinical and clinical development program that, in many c...
Repression of the transcriptional activity of ERRα with sequence-specific DNA-binding polyamides [0.03%]
序列特异性DNA结合聚酰胺对ERRα转录活性的抑制
Chien-Yu Chen,Yang Li,Tiezheng Jia et al.
Chien-Yu Chen et al.
The orphan nuclear receptors estrogen-related receptors (ERRs) bind to the estrogen-related receptor response element (ERRE) to regulate transcriptional programs in cellular metabolism and cancer cell growth. In this study, we evaluated the...
Benzopyrylium salts as new anticancer, antibacterial, and antioxidant agents [0.03%]
苯并吡喃酮盐作为新型抗癌、抗菌和抗氧化剂
Swayamsiddha Kar,Abdul Akhir,Sidharth Chopra et al.
Swayamsiddha Kar et al.
Benzopyrylium salts are an unexplored class of compounds and as a first, this study reports them as potential therapeutic agents. In this effort we pursue the synthesis and in vitro anticancer, antibacterial and antioxidant properties of so...
Synthesis, structure-activity relationship studies and evaluation of a TLR 3/8/9 agonist and its analogues [0.03%]
TLR 3/8/9激动剂及其类似物的合成、结构活性关系研究及评估
Anindya Sarkar,Anushka C Galasiti Kankanamalage,Qian Zhang et al.
Anindya Sarkar et al.
A comprehensive SAR study of a putative TLR 3/8/9 agonist was conducted. Despite the excitement surrounding the potential of the first small molecule TLR3 agonist with a compound that additionally displayed agonist activity for TLR8 and TLR...
Osthole: an overview of its sources, biological activities, and modification development [0.03%]
欧洛石松脂素：来源、生物活性及其结构修饰进展综述
Mingna Sun,Mingjiao Sun,Jianye Zhang
Mingna Sun
Osthole, also known as osthol, is a coumarin derivative found in several medicinal plants such as Cnidium monnieri and Angelica pubescens. It can be obtained via extraction and separation from plants or total synthesis. Plenty of experiment...
Non-acidic bifunctional benzothiazole-based thiazolidinones with antimicrobial and aldose reductase inhibitory activity as a promising therapeutic strategy for sepsis [0.03%]
一类非酸性双功能苯并噻唑基硫唑酮衍生物的抗菌和醛糖还原酶抑制活性在防治脓毒症中的应用前景研究
Antonios Kousaxidis,Lucia Kovacikova,Ioannis Nicolaou et al.
Antonios Kousaxidis et al.
Sepsis is a life-threatening disease that affects millions of people worldwide. Microbial infections that lead to sepsis syndrome are associated with an increased production of inflammatory molecules. Aldose reductase has recently emerged a...