A simple, robust, and affordable bioluminescent assay for drug discovery against infective African trypanosomes [0.03%]
一种简单、稳健且经济的生物发光测定法，用于针对感染性非洲锥虫病的药物发现
Diego Benítez,Estefania Dibello,Mariana Bonilla et al.
Diego Benítez et al.
African trypanosomiasis is a major problem for human and animal health in endemic countries, where it threatens millions of people and affects economic development. New drugs are needed to overcome the toxicity, administration, low efficacy...
Discovery of a novel fluorescent chemical probe suitable for evaluation of neuropilin-1 binding of small molecules [0.03%]
一类新型可供使用的化学荧光探针用于评价小分子与神经纤毛蛋白-1结合状况的研究发现
Daniel Conole,Yi-Tai Chou,Anastasia Patsiarika et al.
Daniel Conole et al.
Neuropilin-1 (NRP1) is emerging as an important molecule in immune signaling where it has been shown to modulate the actions of TGF-β1 in macrophages and regulatory T cells. The development of cost-effective and reliable assays for NRP1 bi...
Comparative Study
Drug development research. 2020 Jun;81(4):491-500. DOI:10.1002/ddr.21641 2020
Development and characterization of oxaceprol-loaded poly-lactide-co-glycolide nanoparticles for the treatment of osteoarthritis [0.03%]
用于治疗骨关节炎的载有oxaceprol的聚乳酸-羟基乙酸纳米颗粒的开发与表征
Emine Alarçin,Çağlar Demirbağ,Seher Karsli-Ceppioglu et al.
Emine Alarçin et al.
Oxaceprol is well-defined therapeutic agent as an atypical inhibitor of inflammation in osteoarthritis. In the present study, we aimed to develop and characterize oxaceprol-loaded poly-lactide-co-glycolide (PLGA) nanoparticles for intra-art...
Selected pharmacotherapy agents as antiproliferative and anti-inflammatory compounds [0.03%]
几种药物作为抗增殖和抗炎化合物的作用研究
Mthanna AlKhalil,Yusuf Al-Hiari,Violet Kasabri et al.
Mthanna AlKhalil et al.
The repurposing of safe therapeutic drugs has emerged as an alternative approach to rapidly identify effective, safe, and conveniently available therapeutics to treat/prevent cancer. Therefore, it was hypothesized that acidic chelator drugs...
Comparative Study
Drug development research. 2020 Jun;81(4):470-490. DOI:10.1002/ddr.21640 2020
Novel 3-aryl-5-substituted-coumarin analogues: Synthesis and bioactivity profile [0.03%]
新型3-芳基-5-取代香豆素衍生物的合成及活性研究
Eleni Kavetsou,Annita Katopodi,Letta Argyri et al.
Eleni Kavetsou et al.
Eighteen 3-aryl-5-substituted-coumarins-six 5-acetyloxy-derivatives, six 5-hydroxy-derivatives, and six 5-geranyloxy-derivatives-were synthesized, structurally characterized and their antioxidant activity, lipoxygenase inhibitory ability, a...
Synthesis of novel flexible tamoxifen analogues to overcome CYP2D6 polymorphism and their biological evaluation on MCF-7 cell line [0.03%]
合成新型柔性的他莫昔芬类似物以克服CYP2D6多态性及其在MCF-7细胞系中的生物评价
Nermin S Ahmed,Jannette Wober
Nermin S Ahmed
Tamoxifen (TAM) is currently the endocrine treatment of choice for all stages of breast cancer; it has proven success in ER positive and ER negative patients. TAM is activated by endogenous CYP450 enzymes to the more biologically active met...
Comparative Study
Drug development research. 2020 Jun;81(4):444-455. DOI:10.1002/ddr.21637 2020
Raghunandan Yendapally,Donald Sikazwe,Subin S Kim et al.
Raghunandan Yendapally et al.
Diabetes mellitus is a serious metabolic disorder affecting millions of people worldwide. Phenformin and metformin are biguanide antidiabetic agents that are conveniently synthesized in a single-step chemical reaction. Phenformin was once u...
Opportunities and challenges of using five-membered ring compounds as promising antitubercular agents [0.03%]
五元环化合物作为抗结核药物的机遇与挑战
Mi Yan,Linlin Xu,Yinhu Wang et al.
Mi Yan et al.
Tuberculosis (TB), a chronic infectious disease, is one of the greatest risks to human beings and 10 million people were diagnosed with TB and 1.6 million died from this disease in 2017. In addition, with the emergence of multidrug-resistan...
Oxalomalate regulates the apoptosis and insulin secretory capacity in streptozotocin-induced pancreatic β-cells [0.03%]
草酸苹果酸对链脲佐菌素诱导的胰岛β细胞凋亡及胰岛素分泌能力的影响
Suping Xin,Xinhua Ye
Suping Xin
Diabetes mellitus (DM) is a kind of metabolic disorder characterized by long-term hyperglycemia. Oxidative stress is involved in inducing the apoptosis of pancreatic β-cells and promoting the development of DM. Oxalomalate (OMA) is a compe...
Investigation of a new horizon antifungal activity with enhancing the antimicrobial efficacy of ciprofloxacin and its binary mixture via their encapsulation in nanoassemblies: in vitro and in vivo evaluation [0.03%]
新型抗真菌活性的研究：通过将环丙沙星及其二元混合物封装在纳米组件中增强抗菌效力的体内和体外评价
Sally Abou Taleb,Asmaa Badawy Darwish,Amira Abood et al.
Sally Abou Taleb et al.
The main goal of this study was to prepare and evaluate nanosponges containing ciprofloxacin (CIP) or its binary mixture with N-acetyl carnosine (NAC). Nanosponges were prepared by ultrasound-assisted synthesis technique using hydroxypropyl...
Comparative Study
Drug development research. 2020 May;81(3):374-388. DOI:10.1002/ddr.21632 2020