Chalcones inhibit firefly bioluminescence dependent on A and B-ring substitution pattern - a structure-activity study combined with molecular docking [0.03%]
flavone衍生物对萤火虫发光的抑制作用及结构活性关系和分子对接研究
Corinna Urmann,Michael Kirchinger,Herbert Riepl
Corinna Urmann
Chalcones represent a privileged scaffold in medicinal chemistry, with pyranochalcones, featuring an additional chromane-like ring, identified as neurogenic and neuroprotective. Reporter gene assays, often used to study these and other effe...
Yaxin Hou,Zhiguang Fu,Chenhui Wang et al.
Yaxin Hou et al.
27-Hydroxycholesterol (27HC), a cholesterol metabolite, functions both as a selective oestrogen receptor (ER) modulator and a ligand for liver X receptors (LXRs). The discovery of 27HC involvement in carcinogenesis has unveiled new research...
Design and synthesis of 1,4,8-triazaspiro[4.5]decan-2-one derivatives as novel mitochondrial permeability transition pore inhibitors [0.03%]
新型线粒体渗透性转过渡孔道抑制剂1,4,8-三氮杂螺[4.5]癸-2-酮类衍生物的设计与合成
Valentina Albanese,Gaia Pedriali,Martina Fabbri et al.
Valentina Albanese et al.
Ischaemia/reperfusion injury (IRI) is a condition that occurs when tissues from different organs undergo reperfusion following an ischaemic event. The mitochondrial permeability transition pore (mPTP), a multiprotein platform including stru...
Synthesis, in vitro and in silico studies of a novel chrysin-ferrocene Schiff base with potent anticancer activity via G1 arrest, caspase-dependent apoptosis and inhibition of topoisomerase II [0.03%]
一种新型的香豆素-铁催化剂席夫碱的合成及其体内外研究：通过G1停滞、caspase依赖性凋亡和抑制拓扑异构酶II展现出了强大的抗癌活性
Mohammed Khaled Bin Break,Siddique Akber Ansari,Ahmed A Katamesh et al.
Mohammed Khaled Bin Break et al.
A novel chrysin-ferrocene Schiff base (CFSB) was synthesised as a potential anticancer agent. CFSB demonstrated high cytotoxicity against cancer cells with HepG2 (liver) being the most susceptible (IC50 = 3.11 µM). The compound was less to...
Identification of broad-spectrum Mpro inhibitors: a focus on high-risk coronaviruses and conserved interactions [0.03%]
广谱Mpro抑制剂的识别：重点是高风险冠状病毒和保守作用方式
Man Liu,Li Zhao,Xupeng Huang et al.
Man Liu et al.
The COVID-19 pandemic underscores the urgent need to develop broad-spectrum antivirals against coronaviruses (CoVs) to prepare for future outbreaks. In this study, we presented a systematic approach to developing broad-spectrum Mpro inhibit...
Structural isomerisation affects the antitubercular activity of adamantyl-isoxyl adducts [0.03%]
结构异构化影响adamantyl-isoxyl加合物的抗结核活性
Yucheng Lu,Daniel Partleton,Filibus M Gugu et al.
Yucheng Lu et al.
Despite efforts to discover effective treatments to eradicate tuberculosis (TB), it remains a global threat. The increase in drug-resistant bacterial species has made the discovery of new drugs highly coveted. The utilisation of previous ef...
Design, synthesis and biological evaluation of novel urolithin derivatives targeting liver cancer cells [0.03%]
新型尿石素衍生物的设计、合成及抗肝癌细胞活性评价
Mi Tian,Lirong Zhao,Yu Lan et al.
Mi Tian et al.
We designed and synthesised 22 new urolithin derivatives (UDs) based on methyl-urolithin A (mUA) to identify anti-cancer drugs with high efficacy and low toxicity and evaluated their anti-cancer activities in vitro. Cytotoxicity tests were ...
Natural product sennoside B disrupts liquid-liquid phase separation of SARS-CoV-2 nucleocapsid protein by inhibiting its RNA-binding activity [0.03%]
大黄酚通过抑制SARS-CoV-2核蛋白的RNA结合活性来干扰其液-液相分离
Da-Wei Zhang,Xiao-Shuang Xu,Liangxu Xie et al.
Da-Wei Zhang et al.
The nucleocapsid protein (NP) of SARS-CoV-2, an RNA-binding protein, is capable of undergoing liquid-liquid phase separation (LLPS) during viral infection, which plays a crucial role in virus assembly, replication, and immune regulation. In...
Activity guided discovery of dual inhibitors of α-glucosidase and β-glucuronidase from the leaves of Millettia pachycarpa Benth [0.03%]
基于活性导向的毛脉紫藤叶中α-糖苷酶和β-葡萄糖醛酸酶双靶点抑制剂的研究
Yanxi He,Huanran Xu,Shaoqian Tan et al.
Yanxi He et al.
Type 2 diabetes mellitus (T2DM) and cancers are two globally prevalent diseases which can increase the incidence of each other. Intestinal α-glucosidase and β-glucuronidase are key targets for glycaemic control and chemotherapy detoxifica...