Novel (Z)-3-(2-(quinazolin-4-yloxy)phenyl)acrylates as potential EGFR inhibitors deriving from the renovation of coumarin skeletons: Design, synthesis, characterization and antineoplastic activity [0.03%]
新型（Z）-3-（2-（喹唑啉-4-基氧）苯基）丙烯酸酯作为EGFR抑制剂的潜在药物：源于香豆素骨架改造的设计、合成、表征及抗肿瘤活性研究
Ruiying Wang,Siqi Wang,Xiaona Ren et al.
Ruiying Wang et al.
The inhibitors of epidermal growth factor receptor (EGFR) have emerged as one of fastest-growing medications that are widely utilized to control the spread and proliferation of malignant tumors. Based on the structural features of quinazoli...
Design, synthesis, and biological evaluation of novel multifunctional caffeic acid-piperazine derivatives for the management of Alzheimer's disease [0.03%]
新型 caffeic 酸-哌嗪 衍生物 的 设计 、 合成 及 生物 学评价： 用于 管理阿尔茨海默病
Sunil Kumar,Neeraj Kumar,Sairam Krishnamurthy et al.
Sunil Kumar et al.
Alzheimer's disease (AD), the most prevalent form of dementia, is marked by progressive memory impairment, cognitive decline, reduced acetylcholine level, oxidative stress, amyloid-β (Aβ) aggregation, and disturbances in metal homeostasis...
Design, synthesis, and evaluation of 4-(aminomethyl)-2-(phenylamino)pyridine derivatives as novel lysyl oxidase-like 2 inhibitors against metastatic melanoma [0.03%]
设计、合成和评估4-（氨基甲基）-2-（苯胺）吡啶衍生物作为新型lysyl氧化酶类似物2抑制剂以对抗转移性黑色素瘤
Geng Yu,Yaoren Qiu,Jie Xie et al.
Geng Yu et al.
Despite extensive validation of lysyl oxidase-like 2 (LOXL2) as a therapeutic target in metastatic cancer, there have been few therapeutic applications of corresponding inhibitors until now. Herein, we reported the design, synthesis, and bi...
A sustainable approach to 1,3-Oxathiolan-5-ones and their identification as a new anthelmintic scaffold [0.03%]
可持续的1,3-氧硫杂环戊酮的方法及其作为新型抗蠕虫化合物的研究
Fernando J Lorenzo,Tania V Veuthey,María José De Rosa et al.
Fernando J Lorenzo et al.
We report an efficient and sustainable solvent-free microwave protocol for the synthesis of a diverse library of 1,3-oxathiolan-5-ones from aromatic, aliphatic, and sugar-derived aldehydes. The method requires no catalysts or organic solven...
Discovery and evaluation of SIPI11594: a novel mitochondrial pyruvate carrier inhibitor with anti-hair loss efficacy [0.03%]
SIPI11594的发现及评价：一种治疗脱发的新颖线粒体丙酮酸载体抑制剂
Han Zhang,Xingyu Wu,Yilei Huang et al.
Han Zhang et al.
Inhibition of the mitochondrial pyruvate carrier (MPC) is a promising strategy to promote hair follicle stem cell activation via lactate production for treating alopecia. To identify new MPC inhibitors, we designed and synthesized 32 novel ...
Discovery of a novel covalent allosteric site CYS434 in Keap1 and its ligand for the treatment of acute lung injury [0.03%]
凯因1新型共价别构位点半胱氨酸434的发现及其配体在治疗急性肺损伤中的应用
Ying Shi,Xin Tie,Guojing Tao et al.
Ying Shi et al.
Keap1 is a central negative regulator of the Nrf2 antioxidant pathway, yet its covalent allosteric modulation remains incompletely understood. Here, we provide evidence that Cys434 may represent a previously unrecognized covalent allosteric...
Evaluation of the meroterpenoids callistrilone O, E and their epimers as potent antiausterity agents [0.03%]
评估紫穗槐松二醇O、E及其差向异构体作为强力抗吝啬剂的效果
Kensuke Okuda,Akira Takagi
Kensuke Okuda
This structure activity relationship study reports the synthesis and evaluation of the meroterpenoids callistrilone O, E, their epimers at the 4-benzylic position, and their pentacyclic precursors as antiausterity agents to starvation-toler...
An HOCl-activated chemiluminescent prodrug enabling self-reporting camptothecin release and imaging-guided therapy in peritoneal metastasis [0.03%]
一种激活HOCl的化学发光前药，可在腹膜转移中自报告喜树碱释放和影像引导治疗
Yanhan Zhou,Hongchao Wang,Maocheng Yang et al.
Yanhan Zhou et al.
Prodrug strategies that exploit tumor-microenvironment abnormalities can enable spatiotemporally controlled chemotherapy; however, most prodrugs are intrinsically silent and cannot report their activation in vivo. We designed and synthesize...
O4-Modified thymidine analogues with photolabile o-nitrobenzyl group derivatives for modulating polymerase primer extension reaction [0.03%]
一种用于调节聚合酶引物延伸反应的含光解o-硝基苄基衍生物的O4-修饰胸腺嘧啶类似物
Ritsuki Sugiura,Hidenori Okamura,Naohiro Yonezawa et al.
Ritsuki Sugiura et al.
Photocaging has emerged as a robust and versatile strategy for achieving precise spatiotemporal control of complex biological processes through UV-induced photoactivation. Here, we sought to develop molecules that allow highly controlled mo...
Design and therapeutic landscape of copper ionophores: From coordination chemistry to cuproptosis modulation [0.03%]
铜离子载体的设计与治疗景观：从配位化学到杯硫调控
Hongmin Zhang,Jiali Xu,Chonglu Li et al.
Hongmin Zhang et al.
Copper ionophores have evolved from serendipitous discoveries into rationally designed therapeutics following the elucidation of cuproptosis. This review analyzes the core design principles that govern ionophore functions, focusing on the d...