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  1. Article ; Online: Naphtho[1,8-ef]isoindole-7,8,10(9H)-trione as novel theranostic agents for photodynamic therapy and multi-subcellular organelles localization.

    Tan, Shaoying / Fu, Qiqi / Lei, Kecheng / Mei, Wenyi / Liu, Jianwen / Qian, Xuhong / Xu, Yufang

    ChemMedChem

    2024  , Page(s) e202400187

    Abstract: A series of naphtho[1,8-ef]isoindole-7,8,10(9H)-trione as novel theranostic agents for photodynamic therapy and multi-subcellular organelles localization were designed and synthesized. Most of them possess moderate fluorescence quantum yield and long ... ...

    Abstract A series of naphtho[1,8-ef]isoindole-7,8,10(9H)-trione as novel theranostic agents for photodynamic therapy and multi-subcellular organelles localization were designed and synthesized. Most of them possess moderate fluorescence quantum yield and long wavelength absorption simultaneously, these made them possible for dual effects of imaging and therapy. Especially, 7b and 7d exhibited significant light-toxicity but slight dark-toxicity. Confocal fluorescence microscopy experiments demonstrated that 7b can locate and image in special multi-subcellular organelles. All the research results implied that carbonyl-phenalene-2,3-dicarboximides derivatives can be applied as a new series of theranostic agents with the characteristics of photodynamic therapy and multi-subcellular organelles imaging.
    Language English
    Publishing date 2024-05-06
    Publishing country Germany
    Document type Journal Article
    ZDB-ID 2218496-X
    ISSN 1860-7187 ; 1860-7179
    ISSN (online) 1860-7187
    ISSN 1860-7179
    DOI 10.1002/cmdc.202400187
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Zs.A 6280: Show issues Location:
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  2. Article ; Online: A simple monoselective C-H oxygenation approach for the synthesis of ursane triterpenoids.

    Mei, Wenyi / Fan, Sisi / Han, Yufei / Shi, Cunjian / Qiu, Lijie / Shen, Yunheng / Zhao, Zhenjiang / Xu, Yufang / Li, Honglin

    Organic & biomolecular chemistry

    2023  Volume 21, Issue 7, Page(s) 1395–1398

    Abstract: Herein, we presented a simple approach for C-H oxidation in the C23 or/and C24 of ursane triterpenoids without any protection of a ... ...

    Abstract Herein, we presented a simple approach for C-H oxidation in the C23 or/and C24 of ursane triterpenoids without any protection of a Δ
    MeSH term(s) Triterpenes/pharmacology ; Triterpenes/chemistry ; Pentacyclic Triterpenes ; Biological Products/chemistry
    Chemical Substances Triterpenes ; ursane ; Pentacyclic Triterpenes ; Biological Products
    Language English
    Publishing date 2023-02-15
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2097583-1
    ISSN 1477-0539 ; 1477-0520
    ISSN (online) 1477-0539
    ISSN 1477-0520
    DOI 10.1039/d3ob00016h
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article ; Online: Anti-inflammatory Effects of a Small Molecule Gastrin-Releasing Peptide Receptor Antagonist on Adjuvant-Induced Rheumatoid Arthritis in Rats.

    Mei, Wen-Yi / Yu, Ming-Jun / Yao, Sen / Wang, Kui-Ling / Yao, Ri-Sheng

    Chemical & pharmaceutical bulletin

    2018  Volume 66, Issue 4, Page(s) 410–415

    Abstract: The anti-inflammatory effects of (R)-2-(1H-Imidazol-1-yl) ethyl-3-(1H-indol-3-yl)-2-(2-p-tolylacetamido)propanamide (RH-1402), a previous designed small molecule Gastrin releasing peptide (GRP) antagonist were evaluated in adjuvant-induced arthritic ... ...

    Abstract The anti-inflammatory effects of (R)-2-(1H-Imidazol-1-yl) ethyl-3-(1H-indol-3-yl)-2-(2-p-tolylacetamido)propanamide (RH-1402), a previous designed small molecule Gastrin releasing peptide (GRP) antagonist were evaluated in adjuvant-induced arthritic model of rats, and the inhibitory effect on neutrophil migration induced by GRP was determined by a transwell system experiment in vitro. The arthritis was induced by injection of Complete Freund's Adjuvant (CFA) containing 10 mg/mL of heat killed mycobacterium into the left hind footpad. Experimental rats were randomly divided into 6 groups, including control, placebo, positive control group, RH-1402 of low/middle/high dose group. Disease incidence and severity was evaluated through scoring of the paw edema and histologic features of joint synovial. Blood of all experimental rats was collected for interleukin 1β (IL-1β) and tumor necrosis factor α (TNF-α) cytokine levels. A transwell system was used to investigate whether RH-1402 would inhibit neutrophils migrating up a gradient of GRP in vitro. RH-1402 (5 and 10 mg/kg) significantly decreased adjuvant induced increased arthritis index during the administration period (days 14-20). Significant inhibition of joint synovial histological features can be found in the RH-1402 treated group, including alleviated Hyperplasia, Inflammatory of infiltration and activation of pannus formation. It also suppressed TNF-α and IL-1β level. Five and 10 mg/kg of RH-1402 significantly inhibited the effect of GRP on neutrophil migration with a dose dependent relationship. These findings indicate that RH-1402 have potential protective anti-inflammatory effects on experimental models of arthritis.
    MeSH term(s) Animals ; Anti-Inflammatory Agents, Non-Steroidal/chemical synthesis ; Anti-Inflammatory Agents, Non-Steroidal/chemistry ; Anti-Inflammatory Agents, Non-Steroidal/pharmacology ; Arthritis, Experimental/chemically induced ; Arthritis, Experimental/drug therapy ; Arthritis, Experimental/pathology ; Freund's Adjuvant/administration & dosage ; Rats ; Rats, Sprague-Dawley ; Receptors, Bombesin/antagonists & inhibitors ; Small Molecule Libraries/chemical synthesis ; Small Molecule Libraries/chemistry ; Small Molecule Libraries/pharmacology
    Chemical Substances Anti-Inflammatory Agents, Non-Steroidal ; Receptors, Bombesin ; Small Molecule Libraries ; Freund's Adjuvant (9007-81-2)
    Language English
    Publishing date 2018-04-01
    Publishing country Japan
    Document type Journal Article
    ZDB-ID 213307-6
    ISSN 1347-5223 ; 0009-2363
    ISSN (online) 1347-5223
    ISSN 0009-2363
    DOI 10.1248/cpb.c17-00887
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 770: Show issues Location:
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    Jg. 1995 - 2021: Lesesall (1.OG)
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  4. Article ; Online: Discovery and optimization of 4-anilinoquinazoline derivatives spanning ATP binding site and allosteric site as effective EGFR-C797S inhibitors.

    Dou, Dou / Wang, Jie / Qiao, Yunjin / Wumaier, Gulinuer / Sha, Wenjie / Li, Wenjie / Mei, Wenyi / Yang, Tingyuan / Zhang, Chen / He, Huan / Wang, Caolin / Chu, Linna / Sun, Baihui / Su, Rongrong / Ma, Xiangyu / Gong, Mengdie / Xie, Lijuan / Jiang, Wenzhe / Diao, Yanyan /
    Zhu, Lili / Zhao, Zhenjiang / Chen, Zhuo / Xu, Yufang / Li, Shengqing / Li, Honglin

    European journal of medicinal chemistry

    2022  Volume 244, Page(s) 114856

    Abstract: Epidermal growth factor receptor (EGFR) is an effective drug target for the treatment of non-small cell lung cancer (NSCLC). However, a tertiary point mutation (C797S) at the ATP binding pocket of the EGFR induces resistance to the third-generation EGFR ... ...

    Abstract Epidermal growth factor receptor (EGFR) is an effective drug target for the treatment of non-small cell lung cancer (NSCLC). However, a tertiary point mutation (C797S) at the ATP binding pocket of the EGFR induces resistance to the third-generation EGFR inhibitors, due to the loss of covalent interaction with Cys797. Here, we designed a series of 4-anilinoquinazoline derivatives that simultaneously occupied the ATP binding pocket and the allosteric site. The newly-synthesized compounds displayed high potency against EGFR-C797S resistance mutation. Among them, compound 14d presented high anti-proliferative effect against BaF3-EGFR
    MeSH term(s) Humans ; Adenosine Triphosphate/metabolism ; Allosteric Site ; Binding Sites ; Carcinoma, Non-Small-Cell Lung/drug therapy ; Cell Line, Tumor ; Drug Resistance, Neoplasm ; ErbB Receptors/antagonists & inhibitors ; ErbB Receptors/genetics ; Lung Neoplasms/drug therapy ; Lung Neoplasms/genetics ; Mutation ; Protein Kinase Inhibitors/chemistry ; Protein Kinase Inhibitors/pharmacology ; Aniline Compounds/chemistry ; Aniline Compounds/pharmacology ; Quinazolines/chemistry ; Quinazolines/pharmacology ; Drug Discovery
    Chemical Substances Adenosine Triphosphate (8L70Q75FXE) ; anilinoquinazoline ; EGFR protein, human (EC 2.7.10.1) ; ErbB Receptors (EC 2.7.10.1) ; Protein Kinase Inhibitors ; Aniline Compounds ; Quinazolines
    Language English
    Publishing date 2022-10-17
    Publishing country France
    Document type Journal Article
    ZDB-ID 188597-2
    ISSN 1768-3254 ; 0009-4374 ; 0223-5234
    ISSN (online) 1768-3254
    ISSN 0009-4374 ; 0223-5234
    DOI 10.1016/j.ejmech.2022.114856
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Zs.B 784: Show issues Location:
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