EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
·
2025
·
IF 5.9
Lidong Gong,Zichao Liang,Xianling Ning,Jianan He,Junjie Huang,Runtao Li,Yuxin Yin,Ridong Li,Zhiqiang Lin
A series of novel 2,4-diarylaminopyrimidine derivatives incorporating a 3-sulfamoylbenzamide moiety were designed and synthesized as potent focal adhesion kinase (FAK) inhibitors. Three compounds ( 5f, 10b , and 10c ) demonstrated FAK inhibitory activities comparable to the reference inhibitor TAE226 . In cellular assays, most analogues exhibited significant antiproliferative effects against four FAK-overexpressing tumor cell lines (HCT116, HeLa, MDA-MB-231, and A375), with IC 50 values below 1 μM. Notably, compound 10c displayed superior potency, showing IC 50 values ranging from 0.08 to 0.31 μM across the tested cell lines, and exhibited approximately 2-fold enhanced activity over TAE226 in inhibiting HCT116, MDA-MB-231, and A375 cell proliferation. Further mechanistic studies revealed that 10c effectively suppressed colony formation, migration, and adhesion of HCT116 cells, while inducing apoptosis via ROS elevation. Molecular docking analysis suggested that the enhanced activity of 10c may arise from an additional hydrogen bond interaction with the Arg426 residue of FAK, leading to stronger binding affinity compared to TAE226 . In vivo , 10c showed good oral bioavailability and significantly inhibited HCT116 xenograft tumor growth (TGI = 62.22 % at 50 mg/kg), outperforming TAE226 (50.98 %) without inducing weight loss or hepatorenal toxicity. These results highlight 10c as a promising FAK-targeted candidate worthy of further preclinical investigation.
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PubMed
高影响因子
ChemistrySelect
·
2026
·Vol. 11
·期 28
·e73876
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IF 2.3
Tao Liu,Huichao Zhang,Bo Huang,Shitong Li,Bin Liu
Mn 2+ -doped perovskite nanocrystals (NCs) have attracted extensive research interest and have been synthesized with sizes in the strong confinement regime. Nevertheless, the size of the doped NCs is still not as small as that of undoped perovskite NCs. To address this, we develop a ligand-assisted reprecipitation method incorporating ultrasonication to synthesize Mn 2+ -doped CsPb(Cl/Br) 3 NCs. The obtained spherical NCs have an average size of 3.1 nm and exhibit orange photoluminescence originating from the 4 T 1 to 6 A 1 transition of Mn 2+ . The luminescent properties correlate with the volume ratio of MnCl 2 to PbBr 2 precursors. Increasing the ratio enhances the Mn 2+ -related emission, while excessive doping leads to photoluminescence quenching. When the precursor ratio is reduced to 1:1, the NCs exhibit both intrinsic exciton and Mn 2+ -related emission, with some particles adopting cubic or rod-like morphologies. Prolonged ultrasonic treatment does not significantly shift the emission peak of the NCs, but promotes superlattice assembly in small-sized NCs, showing a center-to-center separation of 4.2 nm. Subsequently, altering the precursor addition sequence to introduce MnCl 2 last during ultrasonic preparation yields simultaneous formation of spherical and cubic NCs. Finally, post-synthesis doping of Mn 2+ is achieved. Formation of small spherical NCs confirms hypothesis that MnCl 2 induces morphological transformation of NCs. Graphical Ultrasonication-assisted ligand-assisted reprecipitation delivers 3.1 nm Mn 2+ -doped CsPb(Cl/Br) 3 nanocrystals with orange emission from the Mn 2+ 4 T 1 → 6 A 1 transition.
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ACS Applied Nano Materials
·
2026
·
IF 5.8
Ying Li,Yaozu Jia,Lili Wu,Hong Gao,Jing Yao
Lithium–sulfur batteries (LSBs) have attracted significant attention due to their high energy density and low cost. However, further progress in this technology is severely hindered by the shuttle effect of lithium polysulfides (LiPSs) and the sluggish redox kinetics of sulfur cathodes. To overcome these challenges, the application of nanocatalysts into the separators of LSBs boosts the LiPS conversion efficiency. In this study, MoOx (2 < x < 3) submicrometer rods with different oxidation levels are fabricated through precise temperature and atmosphere process parameters. The results show that the composite crystal structure material combines the high electrical conductivity of MoO2 with the high catalytic activity of MoO3, and when used to modify the polypropylene separator, it exhibits catalytic activity for the sulfur reduction reaction and the sulfur evolution reaction. The LSBs deliver a discharge specific capacity of 632.8 mAh g–1 at 8 C and maintain stable cycling for 700 cycles at 1 C, with 0.056% capacity decay per cycle. This study provides a pathway for the preparation of bifunctional catalysis with an integrated structure for LSBs.
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Journal of Translational Medicine
·
2026
·Vol. 24
·期 1
·1029
·
IF 9.7
Cheng Kai-wen,Zhou Shao-jun,Zeng Jie,Zhang Yang-rui,Jin Bing-qian,Wang Ping,He Ling-yan,Qi Xu-chen,Liu Xu-dong,Yu Lu-shan,Zhang Yan-xing
Background Among tumors affecting the central nervous system (CNS), glioblastoma multiforme (GBM) is the most aggressive and lethal form. Given the complex mechanisms of the CNS and the blood-brain barrier (BBB), effective therapies for GBM remain limited. To identify potential therapeutic candidates for glioma, we developed a small-molecule library to screen for compounds with potent anti-proliferative effects and BBB permeability. The mechanisms underlying their anti-glioma activity were further elucidated to provide insights into new treatment strategies. Methods A library of small molecules was screened to identify agents that significantly inhibit glioma cells activity. The effects of the lead compound (Dihydrotanshinone I, DHT) on glioma progression were evaluated through a series of experimental approaches, including cell counting kit-8 assays, cell cycle analysis, apoptosis detection, wound healing, transwell migration, reactive oxygen measurement, subcutaneous xenograft mouse models, and intracranial orthotopic tumor models. To elucidate the underlying mechanisms, network pharmacology and transcriptomic analyses were employed. The mechanism of DHT in glioma pathogenesis was further validated using bioinformatics analyses and clinical glioma tissue samples. Results Based on pharmacokinetic evaluation, DHT was found to traverse the BBB, indicating its capacity to reach the cerebral parench. In vitro and in vivo experiments demonstrated that DHT significantly suppresses glioma growth and progression. Mechanistic analyses using network pharmacology and RNA sequencing revealed that DHT induces glioma cell apoptosis by inhibiting the Janus kinase-signal transducer and activator of transcription 3 (STAT3) signaling pathway, increasing intracellular reactive oxygen species levels and triggering intrinsic apoptotic cascades. Furthermore, bioinformatic analyses of clinical cohorts coupled with validation in patient-derived glioma specimens confirmed that elevated STAT3 expression was correlated with unfavorable prognosis and was significantly increased in patients with high-grade glioma. Conclusions This study demonstrates that, in addition to its role as a key contributor to glioma malignancy and a prognostic marker, STAT3 is also a target of DHT, highlighting its potential as a promising therapeutic candidate for treating GBM. Graphical
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高影响因子
ACS Applied Energy Materials
·
2026
·
IF 5.5
Jiaoyang Shen,Hehe Ren,Jian Zou,Xin Guo,Yuanjie Wei,Quancai Li,Jing Liang,Wei Wu
Aqueous symmetric sodium-ion batteries (ASSIBs) are gaining attention as attractive energy storage devices for flexible and wearable electronics due to their excellent structural stability, inherent safety, environmental friendliness, and the abundant sodium resources. NASICON-structured Na2VTi(PO4)3 (NVTP) features a three-dimensional framework structure; Ti4+/Ti3+ and V4+/V3+ redox couples can be used to fabricate symmetrical sodium-ion batteries as both the anode and the cathode. However, poor cycle stability and irreversible dissolution in aqueous solutions limit the application of NVTP in flexible ASSIBs. Herein, the Na1.9K0.1VTi(PO4)3-10% GNP (NKVTP-GNP) composite was synthesized by partially substituting Na+ in Na2VTi(PO4)3 with K+ and coating graphene nanoplatelets (GNP). The K+ doping and GNP coating successfully promoted the conversion of V4+ to V5+ and enhanced the cycling stability of the materials. The capacity retention rate of the NKVTP-GNP cathode is 99% after 1000 cycles, while the anode maintains 81% of its capacity after 500 cycles. Additionally, a flexible symmetric battery NKVTP-GNP//NKVTP-GNP was fabricated via a screen-printing technique, which delivered a wide voltage window of 1.8 V, an energy density of 63 Wh kg−1, and excellent cycling stability, retaining 90% of its capacity after 2000 cycles at 10 C. More importantly, the battery shows high flexibility, adjustable shapes, and high-throughput manufacturing. This work provides insights into the development of high-performance flexible ASSIBs.
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NANO
·
2024
·
IF 1
Jianchao Wang,Ziqi Wu,Huayong Peng
Ordered Ag@Au hybrid nanotube arrays were prepared by a galvanic replacement reaction and subsequently evaluated for their effectiveness as substrates for enhancing the fluorescence of poly(3-hexylthiophene) (P3HT). Ordered AgNWs arrays were assembled using a three-phase interface method, and ordered Ag@Au hybrid nanotube arrays were successfully prepared by a galvanic replacement reaction between a HAuCl 4 solution and ordered AgNWs arrays. The morphology of the ordered silver nanowires (AgNWs) arrays and Ag@Au nanotube arrays, as well as the influence of reaction time on the galvanic replacement reaction, were investigated. The fluorescence and laser-Raman properties of the conjugated polymer P3HT on various ordered Ag@Au nanotubes were analyzed. Gold (Au) particles grow on the surface of AgNWs, the diameter of the nanotubes gradually increases, and the ordered Ag@Au hybrid nanotubes form gradually. The surface plasmon resonance (SPR) peaks of Ag@Au hybrid nanotube arrays redshift and become wider as the reaction proceeds compared to AgNW arrays. The fluorescence properties of P3HT films on various ordered Ag@Au hybrid nanotubes were much higher than those on bare silicon substrates, but compared to the gold nanowire array, there is a decrease. As the galvanic displacement reaction progresses, the degree of reduction in fluorescence intensity increases. The unique aspect of this work was that the plasmon resonance wavelength of the ordered Ag@Au hybrid nanotube arrays showed a substantial redshift and broadening, which is much closer to biological samples. The ordered Ag@Au hybrid nanotube arrays can be used as ultra-sensitive fluorescence sensing platforms.
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高影响因子
ORGANIC PROCESS RESEARCH & DEVELOPMENT
·
2026
·
IF 3.5
Jinnai Liu,Jiawei Tang,Hao Chen,Li Zhang,Ganlan Li,Fuli Zhang,Shaoxin Chen,Jun Yu
(S)-3-Bromo-2-(1-methoxyethyl)pyridine 1 is a key intermediate of RMC-6236. In this report, we detail the development and optimization of a highly enantioselective chemoenzymatic and kilogram-scale process for 1. The developed process for intermediate (S)-1-(3-Bromopyridin-2-yl)ethanol 3 was performed on 1 kg scale with a substrate concentration of 70.0 g/L, achieving a yield of 93.0% and an ee value of >99.9%. Subsequently, a simple and effective NaHMDS/CH3I methylation system afforded the title compound 1, in 95.0% yield and with >99.9% ee, achieving 88.4% overall yield from intermediate 1-(3-bromopyridin-2-yl)ethanone 2. This represents a notable increase compared to the early stage process (overall yield 55.5%). This optimized highly efficient and sustainable process was demonstrated during kilogram-scale production of 1.
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高影响因子
Nanoscale
·
2026
·
IF 5.2
Tingting Cai,Shuangshuang Zhao,Qin Fang,Huixin Chen,Xiuli Jia,DONGXU YU
Vanadium (III) oxide (V2O3) has emerged as a promising cathode material for aqueous zinc-ion batteries owing to high theoretical capacity based on reversible two-electron redox chemistry. However, the cycling stability and reaction kinetics are highly sensitive to its microstructural characteristics, which remain insufficiently understood. Here, we report a facile and scalable synthesis of V2O3 via combining oil-bath reaction and controlled calcination process, enabling precise regulation of particle morphology and microstructure through calcination time. Systematic microstructural evolution is correlated with Zinc-ion storage behavior, revealing that optimized architectures effectively promote ion transport kinetics and structural stability. Coupled with a high-concentration water-in-salt electrolyte to suppress parasitic reactions, the optimized V2O3 cathode delivers a high specific capacity of 453.8 mA h g -1 at 0.05 A g -1 , exceptional rate capability with 180 mA h g -1 retained at 10 A g -1 , and prolonged cycling stability of 210 mAh g -1 after 1000 cycles at 1 A g -1 . This work elucidates the underlying structure-property relationship governed by microstructure but also provides valuable insights into the design of highperformance cathode materials for advanced energy storage systems.
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PubMed
高影响因子
Small
·
2026
·
IF 11.8
Yudian Xu,Huajing You,Linlin Cao,Jun Pu,He Li,Kun Qian,Chao Wu,Wei Xu
Spinocerebellar ataxia type 3 (SCA3) is a progressive inherited neurodegenerative disorder for which accessible blood-based classification approaches are needed. In this retrospective, single-center study, plasma metabolic fingerprints were acquired from 202 participants using mesoporous PdPt nanoparticle-assisted laser desorption/ionization mass spectrometry (LDI-MS) and analyzed using a Tabular Prior-data Fitted Network (TabPFN) classifier. The model achieved AUCs of 0.952 in the discovery cohort and 0.963 in the internal temporal validation cohort. A reduced 21-metabolite panel retained discriminatory performance, with AUCs of 0.901 and 0.932, respectively. Exploratory clinical and pathway analyses provided additional biological context. These findings highlight the potential of PdPt-assisted plasma metabolic fingerprinting for SCA3 classification.
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高影响因子
OPTICAL MATERIALS
·
2026
·
IF 4.3
Zongming Yu,Zuhuan Lu,Yukun Wang,Yuanhao Li,Tianyi Zhang,Wenhong Sun
Improving detector performance through simple doping engineering of hole transport layers. • 3-Bromopyridine, as a dual function dopant of Spiro-OMeTAD, can enhance ion transport and passivate defects to achieve the synergistic optimization of transport and stability. • The device is self-powered, the external quantum efficiency of the device is 90%, the dark current density is reduced by two orders of magnitude, the detection rate is increased to 2.77 × 10 13 Jones, and the linear dynamic range is widened to 168.23 dB. Spiro-OMeTAD (2,2′,7,7′-Tetrakis[N,N-di(4-methoxyphenyl)amino]-9,9′-spirobifluorene) is widely used as the hole-transport layer (HTL) in perovskite optoelectronic devices due to its solution processability and favorable material properties. However, undoped Spiro-OMeTAD exhibits inherently low electrical conductivity, necessitating dopants such as lithium bis(trifluoromethanesulphonyl)imide (Li-TFSI) to enhance its charge transport properties. Nevertheless, Li-TFSI possesses strong hygroscopicity and is prone to aggregation within the Spiro-OMeTAD film, which significantly compromises both device performance and stability. To address this challenge, we report a dual-functional strategy that employs 3-Bromopyridine (3-BP) as a dopant to simultaneously enhance hole transport and provide interfacial passivation in Spiro-OMeTAD HTLs. The pyridine nitrogen atom in 3-BP coordinates with Li + ions, weakening Li + –TFSI - interactions and consequently enhancing the mobility of TFSI − anions and the overall film conductivity. Simultaneously, the bromine atom forms halogen bonds with the methoxy oxygen atoms of Spiro-OMeTAD, which strengthens intermolecular interactions and passivates defects. Optimal doping at 2 wt% 3-BP leads to significant performance enhancements: the external quantum efficiency (EQE) increases from 82% to 90%, the dark current density (J d ) decreases by two orders of magnitude (from 7.46× 10 −8 A/cm 2 to 8.71 × 10 −10 A/cm 2 ), and the stability is enhanced, retaining 83.77% of its initial EQE after 500 h of unencapsulated storage in ambient air.
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高影响因子
APPLIED SURFACE SCIENCE
·
2026
·
IF 6.6
Lirong Yang,Hui Li,Fubao Zhang,Xun Wang,Xiaona Zhai,Yin Qiao,Haixia Qi,Haoyuan You,Feng Liu
A hierarchical 3-tier architecture was constructed on the surface of zwitterionic M1 / M2 membranes. • M1 and M2 membranes showed excellent antifouling performance with FRR reaching 93.75 % and 95.93 %. • M1 and M2 membranes showed good anticoagulant activity with PRT reaching 28.9 and 32.1 min. • M1 and M2 membranes showed low immune response with C5a decreasing to 1.62 and 1.31 ng/mL. Although polyethersulfone (PES) ultrafiltration membranes possess good thermal stability, mechanical stability, and biocompatibility, their inherent hydrophobicity leads to severe organic fouling and flux decline. Herein, a synergistic modification strategy combining fluorination and zwitterionization is proposed to address this issue. A three-tier hierarchical structure was constructed on the surfaces of the M1 and M2 membranes, consisting of an outer zwitterion-induced highly hydrophilic hydration layer, an intermediate CF 3 -induced hydrophobic low-surface-energy lubricious layer, and an underlying imidazole N–H-induced hydrogen-bonded hydration layer. This unique surface design endows the membrane surface with a biointerface featuring high permeability, low fouling, and hemocompatibility. Compared with the pristine PES membrane (M0), the M1 and M2 membranes exhibit significantly enhanced pure water flux (271.6 and 292.0L m −2 h −1 , respectively, vs. 241.1 L m −2 h −1 for M0), substantially reduced bovine serum albumin adsorption (30.56 and 17.67μg cm −2 , respectively, vs. 171.98μg cm −2 for M0), as well as markedly suppressed erythrocyte and platelet adhesion, with antibacterial adhesion efficiency exceeding 90 % for both membranes. Hemocompatibility tests further demonstrate that the zwitterionic membranes achieve hemolysis ratios as low as 0.39 % and 0.34 %, respectively, along with favorable anticoagulant properties and the ability to inhibit complement activation. A hierarchical 3-tier architecture constructed by zwitterionic fluorinated PES provides a promising solution to create excellent biointerface for heavily used UF membranes. Download: Download high-res image (145KB) Download: Download full-size image
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高影响因子
Surfaces and Interfaces
·
2026
·
IF 6
Suping Jia,Xinyu Chen,Yan Zhou,Jie Jiang,Huinian Zhang,Yujuan Zhang,Qing Chang
The main challenge of applying low-temperature-prepared TiO 2 (LTP-TiO 2 ) to perovskite solar cells lies in its high density of defect states, which adversely affects electron transport at the interface and within the electron transport layer. Through strategic utilization of the ionic liquid 1-ethyl-3-methylimidazolium acetate (EMIMAc), we developed an effective approach to passivate defect states of LTP-TiO 2 and enhance electron transport dynamics in perovskite photovoltaic devices. This ionic liquid additive simultaneously suppresses non-radiative recombination and improves electron extraction efficiency at the perovskite/TiO 2 interface. The EMIMAc-modified TiO 2 demonstrates an optimized electron mobility of 4.16×10 −5 cm²·υ⁻¹·s⁻¹, yielding a higher power conversion efficiency (PCE) of 21.03% with superior stability, thus marking a substantial enhancement over unmodified devices. Download: Download high-res image (212KB) Download: Download full-size image Ionic liquid 1-ethyl-3-methylimidazolium acetate (EMIMAc) possesses an acetate anion that can strongly coordinate with under-coordinated Ti 4+ sites and passivate oxygen vacancies on the TiO 2 surface, while the imidazolium cation interacts with the perovskite to suppress interfacial defects. It can simultaneously suppress non-radiative recombination, improve charge extraction efficiency at the perovskite/TiO 2 interface and enhance the electron mobility of TiO 2 . A high efficiency of 21.03% with negligible hysteresis, improved stability was obtained when used low-temperature-processed TiO 2 as electron transport material in perovskite solar cells.
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高影响因子
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