Genome mining and metabolomics unveil new napyradiomycin antibiotics from Streptomyces sp. 0H2M [0.03%]
基因组数据挖掘和代谢组学揭示链霉菌新产生奈派雷霉素抗生素
Min Wang,Nuo Chen,Qichen Zhang et al.
Min Wang et al.
Napyradiomycins are a family of meroterpenoid natural products known for their promising antibiotic activities. In this study, four new napyradiomycins derivatives were identified, SF2415B4 (1), SF2415B5 (2), SF2415B6 (3), and SF2415B7 (4) ...
Chemoenzymatic assembly of structurally defined heparan sulfate oligosaccharides reveals heparanase substrate plasticity and enables inhibitor design [0.03%]
结构明确的硫酸肝糖寡糖的化学生物合成可揭示肝素酶底物的多样性和使设计抑制剂成为可能
Xiao Wang,Qinyu Liu,Guijiao Zhang et al.
Xiao Wang et al.
Heparanase (HPSE) is a promising therapeutic target, yet current heparin-derived inhibitors are limited by structural heterogeneity, poor selectivity, and off-target anticoagulant effects. Here, we synthesized a library of structurally defi...
Alkaloids from the nearly ripe fruits of Tetradium ruticarpum and inhibitory effects on colorectal cancer cells [0.03%]
石防风近成熟果实中的生物碱及其抑制结肠癌细胞增殖的作用
Ping Guo,Yuanyuan Li,Jianming Yu et al.
Ping Guo et al.
Tetradium ruticarpum is a commonly used medicinal herb in China that has been widely applied to alleviate clinical symptoms such as abdominal distension, abdominal pain, vomiting, and diarrhea. In the present study, total alkaloids were pre...
Natural cyclic depsipeptides and their analogs as potential antimicrobial candidates: mechanistic insight [0.03%]
具有抗菌潜力的天然环状肽及其类似物：机制见解
Gautam Kumar,Kritika Engle
Gautam Kumar
Microorganisms such as bacteria, viruses, fungi, and parasites cause serious infections in humans. The misuse of antimicrobial treatments in humans, animals, and agriculture has led to the development of resistant pathogens that can survive...
Heterostructure engineering of Au@UiO-67-bpy(Cu)/MoS2 cascade nanozymes for self-fueled and NIR-enhanced chemodynamic/photothermal cancer therapy [0.03%]
Au@UiO-67-bpy(Cu)/MoS2级联纳米酶异质结构工程用于自驱动和近红外增强的化学动力学/光热癌症治疗
Umarov Abdusalom,Kasimova Gulnora,Alikulova Hakima et al.
Umarov Abdusalom et al.
The development of multifunctional nanozymes capable of integrating catalytic cascade reactions with externally controllable therapeutic activation remains an important challenge in cancer nanomedicine. Herein, we report a heterostructure-e...
Prenylated 4-Hydroxycoumarin derivatives as inducers of CDK4/6-mediated cell cycle arrest: From design and synthesis to in vitro and in vivo evaluation of their anti-breast Cancer activity [0.03%]
设计、合成及体内外评价一系列CDK4/6激活剂-肉桂酰化4-香豆素衍生物作为乳腺癌治疗药物的候选物
Xinyao Pan,Shiyu Wang,Kaifeng Lai et al.
Xinyao Pan et al.
Breast cancer is the most frequently diagnosed malignancy in women, and safer, more effective therapies are urgently needed. Inspired by the prenylated coumarin scaffolds of Ferulin C and Miliusol, we rationally designed and synthesized a s...
The rational design and mechanism study of heterocyclic thioester fungicides based on the bioisosterism strategy [0.03%]
基于生物电子等排策略的杂环硫酯类杀菌剂的合理设计与作用机制研究
Yipeng Wu,Lei Qi,Hongwei Yu et al.
Yipeng Wu et al.
Aiming to develop highly efficient and environmentally friendly fungicides, this study designed and synthesized a series of heteroaromatic thioester compounds (C=O → C=S) using a bioisosterism strategy. In vitro antifungal assays revealed ...
The discovery of potent and selective N6-modified adenosine derivatives as effective chemotherapeutic agents to overcome p53-dependent drug resistance in cancer and HPIV-3/AdV5 respiratory tract infections [0.03%]
一类高效且具有高度选择性的N6修饰的腺苷衍生物能有效克服肿瘤p53依赖性耐药以及HPIV-3/AdV5所致呼吸道感染的化学治疗药物的发现
Elżbieta Speina,Katherine Burchiellaro,Marta Denel-Bobrowska et al.
Elżbieta Speina et al.
A library of N6-modified adenosine derivatives (compounds 7-36) was synthesized via a one-step reaction of 6-chloro- or 2-amino-6-chloro-(β-D-ribofuranosyl)-9H-purine with primary or secondary amines. The structures of selected compounds (...
An affordable and low-waste protocol for rapid and robust solid-phase peptide synthesis at elevated temperatures [0.03%]
一种经济且低浪费的升高温固相肽合成快速而稳健的工艺流程
Giacomo Bettin,Matilde Salvadoretti,Guglielmo Rossi et al.
Giacomo Bettin et al.
Automated solid-phase peptide synthesis (SPPS) is the premier methodology for producing high-purity peptides across a broad range of applications. However, despite its efficiency, automated SPPS often requires expensive instrumentation and ...
Synthesis and evaluation of 3,5-disubstituted isothiazolo[4,5-b]pyridines, pyrazolo[4,3-b]pyridines and isothiazolo[3,4-b]pyrazines as inhibitors of PIKfyve [0.03%]
作为PIKfyve抑制剂的3,5-取代异噻唑并吡啶、吡唑并吡啶和异噻唑并吡嗪类化合物的设计与评价
Ling-Jie Gao,Mathy Froeyen,Chieh-Wen Lo et al.
Ling-Jie Gao et al.
Various 3,5-disubstituted isothiazolo[4,3-b]pyridines were previously shown to be potent inhibitors of the lipid kinase PIKfyve, displaying broad-spectrum antiviral activity. To further study their structure-activity relationship and to dis...