检索结果-南通市图书馆

Bifunctional fluorescent probes for hydrogen peroxide and diols based on a 1,8-naphthalimide fluorophore

在线全文

学校读者我要写书评

暂无评论

Science China Chemistry 2013年第10期56卷 1440-1445页

作者： SUN Wei MA Zhao li Jing li WenHua DU LuPei li minyong Department of Medicinal Chemistry Key Laboratory of Chemical Biology (MOE) School of Pharmacy Shandong University

This report discloses a series of naphthalimide-based bifunctional fluorescent probes for hydrogen peroxide and *** a result,these molecules not only demonstrated high turn-on fluorescent response and good selectivity towards hydrogen peroxide over other relevant reactive oxygen species,but also displayed different responses to ***,these fluorescent probes could be served as sensitive,selective and practical chemosensors for both hydrogen peroxide and diols under physiologicallike conditions.

关键词： 1,8-naphthalimide bifunctional fluorescent probe hydrogen peroxide diols

Design of OFF/ON fluorescent thiol probes based on coumarin fluorophore

在线全文

学校读者我要写书评

暂无评论

Science China Chemistry 2012年第9期55卷 1776-1780页

作者： SUN Wei li Jing li WenHua SU liJuan DU LuPei li minyong Key Laboratory of Chemical Biology of Natural Products(MOE) Department of Medicinal ChemistrySchool of PharmacyShandong UniversityJinan 250012China

This paper presents a series of first- and second-generation click-modified coumarin-based fluorescent probes for thiols. These molecules demonstrate high turn-on fluorescent response and good selectivity towards aromatic thiols over other relevant reac- tive sulfur species, reactive oxygen species and common nucleophiles. Moreover, probe la can detect thiols in the reduced rabbit plasma sample. Therefore, this approach provides a particularly impressive tool for detecting thiol in biological systems.

关键词： coumarin fluorescent probe aliphatic thiols thiophenols

Visualization of α_1-adrenergic receptors with phenylpiperazine-based fluorescent probes

在线全文

学校读者我要写书评

暂无评论

Science China Chemistry 2016年第5期59卷 624-628页

作者： Yuxing lin Wenhua li Qinying Yu Xinyang Zhou Wei Zhang Lupei Du minyong li Key Laboratory of Chemical Biology (Ministry of Education) Department of Medicinal Chemistry School of Pharmacy Shandong University

Several novel fluorescent probes targeting α_1-adrenergic receptors were well designed and synthesized by conjugating phenylpiperazine pharmacophore with coumarin and fluorescein fluorophores. These compounds showed suitable fluorescence property, high receptor affinity, and low cytotoxicity. Moreover, the cell imaging results displayed that these probes can be effective tools for the real-time detection of ligand-receptor interactions, as well as the visualization and location of α_1-adrenergic receptors in living cells.

关键词： α1-adrenergic receptors fluorescent probes high affinity fluorescent imaging

Improved Antiproliferative Activities of a New Series of 1,3,4-Thiadiazole Derivatives Against Human Leukemia and Breast Cancer Cell lines

在线全文

学校读者我要写书评

暂无评论

Chemical Research in Chinese Universities 2016年第5期32卷 768-774页

作者： liU Tingting WAN Yichao liU Renshuai MA lin li minyong FANG Hao Key Laboratory of Chemical Biology Ministry of Education Department of Medicinal Chemistry School of Pharmacy Shandong University Jinan 250012 P. R. China

Twenty-two novel 1,3,4-thiadiazole derivatives were synthesized using different aromatic acids as starting materials, followed by cyclization, coupling and deprotection reaction. The structures of all the target compounds were identified by means of IH nuclear magnetic resonance（NMR）, laC NMR and high resolution mass spectrometer（HRMS）. Further biological evaluations were performed for chronic myelogenous leukemia cell and breast cancer cell. The results suggest that most of the target compounds exhibit potent anti-proliferative activities. Especially, compound 5b shows better antiproliferative activities against MDA-MB-231 and K562 cell lines compared with gossypol.

关键词： Thiadiazole Anti-tumor activity Antiproliferative activity

Environmentally sensitive fluorescent probes with improved properties for detecting and imaging PDEδ in live cells and tumor slices

维普期刊数据库评论

在线全文

维普期刊数据库

学校读者我要写书评

暂无评论

Chinese Chemical Letters 2023年第11期34卷 214-219页

作者： Keliang li Shanchao Wu Gaopan Dong Yu li Wei Wang Guoqiang Dong Zhanying Hong minyong li Chunquan Sheng School of Pharmacy Second Military Medical UniversityShanghai 200433China Department of Medicinal Chemistry Key Laboratory of Chemical Biology(MOE)School of Pharmaceutical SciencesCheeloo College of MedicineShandong UniversityJi’nan 250012China

Kirsten rat sarcoma viral oncogene homolog(KRAS)-phosphodiesterase-delta(PDEδ)is a promising target for antitumor drug ***,highly efficient and environmentally sensitive fluorescent probes of PDEδ(DS-Probes)were rationally *** compared with the reported PDEδprobes,DS-Probes showed higher binding affinity and selectivity,which were able to conveniently and efficiently label PDEδin live cells as well as tumor ***,these fluorescent probes are expected to facilitate PDEδ-based mechanism elucidation,drug discovery and pathologic diagnosis.

关键词： Antitumor PDEδ Fluorescent probes Environmentally sensitive Binding affinity

Identification of anthelmintic parbendazole as a therapeutic molecule for HNSCC through connectivity map-based drug repositioning

在线全文

学校读者我要写书评

暂无评论

Acta Pharmaceutica Sinica B 2022年第5期12卷 2429-2442页

作者： Dong liang Chen Yu Zhao Ma Xingye Yang Zhenzhen li Xuhui Dong Xiaojun Qin Lupei Du minyong li Key Laboratory of Chemical Biology(MOE) School of Pharmaceutical SciencesCheeloo College of MedicineShandong UniversityJinan 250012China

Head and neck squamous cell carcinoma(HNSCC) is one of the most common human cancers;however, its outcome of pharmacotherapy is always very limited. Herein, we performed a batch query in the connectivity map(cMap) based on bioinformatics, queried out 35 compounds with therapeutic potential, and screened out parbendazole as a most promising compound, which had an excellent inhibitory effect on the proliferation of HNSCC cell lines. In addition, tubulin was identified as a primary target of parbendazole, and the direct binding between them was further verified. Parbendazole was further proved as an effective tubulin polymerization inhibitor, which can block the cell cycle, cause apoptosis and prevent cell migration, and it exhibited reasonable therapeutic effect and low toxicity in the in vivo and in vitro anti-tumor evaluation. Our study repositioned an anthelmintic parbendazole to treat HNSCC, which revealed a therapeutic utility and provided a new treatment option for human cancers.

关键词： HNSCC cMap Bioinformatics Parbendazole Drug repositioning Anti-tumor

Multiple rapid-responsive probes for hypochlorite detection based on dioxetane luminophore derivatives

在线全文

学校读者我要写书评

暂无评论

Journal of Pharmaceutical Analysis 2022年第3期12卷 446-452页

作者： Yingai Sun Yuqi Gao Chunchao Tang Gaopan Dong Pei Zhao Dunquan Peng Tiantian Wang Lupei Du minyong li Department of Medicinal Chemistry Key Laboratory of Chemical Biology(MOE)School of PharmacyShandong UniversityJinan250012China School of Pharmaceutical Sciences Sun Yat-sen UniversityGuangzhou510006China State Key Laboratory of Microbial Technology Shandong UniversityJinan250100China

In recent years,various methods for detecting exogenous and endogenous hypochlorite have been studied,considering its essential role as a ***,the existing technologies still pose obstacles such as their invasiveness,high costs,and complicated *** the current study,we developed a glow-type chemiluminescent probe,hypochlorite chemiluminescence probe(HCCL)-1,based on the scaffold of Schaap's 1,2-dioxetane *** better explore the physiological and pathological functions of hypochlorite,we modified the luminophore scaffold of HCCL-1 to develop several probes,including HCCL-2,HCCL-3,and HCCL-4,which amplify the response signal of *** comparing the luminescent intensities of the four probes using the IVIS®system,we determined that HCCL-2 with a limit of detection of 0.166 mM has enhanced sensitivity and selectivity for tracking hypochlorite both in vitro and in vivo.

关键词： Glow-type Chemiluminescent probe 1,2-Dioxetane Hypochlorite

First small-molecule PROTACs for G protein-coupled receptors:inducing α1A-adrenergic receptor degradation

维普期刊数据库评论

在线全文

维普期刊数据库

学校读者我要写书评

暂无评论

Acta Pharmaceutica Sinica B 2020年第9期10卷 1669-1679页

作者： Zhenzhen li Yuxing lin Hui Song Xiaojun Qin Zhongxia Yu Zheng Zhang Gaopan Dong Xiang li Xiaodong Shi Lupei Du Wei Zhao minyong li Department of Medicinal Chemistry Key Laboratory of Chemical Biology(MOE)School of PharmacyShandong UniversityJinan 250012China Department of Immunology Key Laboratory of Infection and Immunity of Shandong ProvinceSchool of Basic Medical ScienceShandong UniversityJinan 250012China Department of Chemistry University of South FloridaTampaFL 33620USA State Key Laboratory of Microbial Technology Shandong UniversityJinan 250100China

Proteolysis targeting chimeras(PROTACs)are dual-functional hybrid molecules that can selectively recruit an E3 ubiquitin ligase to a target protein to direct the protein into the ubiquitinproteasome system(UPS),thereby selectively reducing the target protein level by the ubiquitinproteasome ***,small-molecule PROTACs are gaining popularity as tools to desrade pathogenic ***,we present the first small-molecule PROTACs that can induce the alA-adrenergic receptor(α1 A-AR)degradation,which is also the first small-molecule PROTACs for G proteincoupled receptors(GPCRs)to our *** degradation inducers were developed through conjugation of knownα1-adrenergic receptors(α1-ARs)inhibitor prazosin and cereblon(CRBN)ligand pomalidomide through the different *** representative compound 9 c is proved to inhibit the proliferation of PC-3 cells and result in tumor growth regression,which highlighted the potential of our study as a new therapeutic strategy for prostate cancer.

关键词： Small-molecule PROTACs α1A-Adrenergic receptor Ubiquitylation Degradation Prostate cancer

A specific and selective chemiluminescent probe for Pd^(2+) detection

在线全文

学校读者我要写书评

暂无评论

Chinese Chemical Letters 2019年第1期30卷 63-66页

作者： Yuqi Gao Yuxing lin Tingting liu Xiaomeng Zhang Feng Xu Pan liu Lupei Du minyong li Department of Medicinal Chemistry Key Laboratory of Chemical Biology (MOE) School of Pharmacy Shandong University State Key Laboratory of Microbial Technology Shandong University

As an important transition metal catalyst, palladium is extensively used in many areas including electronics industry, petroleum industry, automobile industry and fine chemicals engineering. However,it brings harm to the environment as well as people's health. Herein, we managed to introduce a butynyl group to 1,2-dioxetane developing a reaction-based chemiluminescent probe as well as an imaging approach for monitoring palladium(II). Exhibiting enhanced total flux in Pd2+enriched areas, palladium chemiluminescent probe(PCL) may afford potential utility for detecting Pd2+in vitro, in cellulo and in vivo.

关键词： Chemiluminescent imaging Chemiluminescence 1,2-Dioxetane Palladium(Ⅱ) Bioassays