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  1. Article ; Online: The Coronavirus Epidemic.

    Hilgeroth, A

    Medicinal chemistry (Shariqah (United Arab Emirates))

    2020  Volume 16, Issue 3, Page(s) 271

    MeSH term(s) Chemistry, Pharmaceutical ; Coronavirus Infections/epidemiology ; Coronavirus Infections/transmission ; Epidemics ; Humans
    Keywords covid19
    Language English
    Publishing date 2020-04-23
    Publishing country Netherlands
    Document type Editorial
    ISSN 1875-6638
    ISSN (online) 1875-6638
    DOI 10.2174/157340641603200226092100
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: Evaluation of Novel Benzo-annelated 1,4-dihydropyridines as MDR Modulators in Cancer Cells.

    Werner, Peter / Szemeredi, Nikoletta / Spengler, Gabriella / Hilgeroth, Andreas

    Anti-cancer agents in medicinal chemistry

    2024  

    Abstract: Background: Multidrug resistance (MDR) is the main problem in anticancer therapy today. Causative transmembrane efflux pumps in cancer cells have been reconsidered as promising anticancer target structures to restore anticancer drug sensitivity by ... ...

    Abstract Background: Multidrug resistance (MDR) is the main problem in anticancer therapy today. Causative transmembrane efflux pumps in cancer cells have been reconsidered as promising anticancer target structures to restore anticancer drug sensitivity by various strategies, including MDR modulators. MDR modulators interfere with the efflux pumps and improve the cellular efficiency of chemotherapeutics. So far, only a few candidates have gone through clinical trials with disappointing results because of low specificity and toxic properties.
    Aim: This study aimed to find Novel MDR modulators to effectively combat multidrug resistance in cancer cells.
    Objective: We synthesized various novel benzo-annelated 1,4-dihydropyridines to evaluate them as MDR modulators towards ABCB1 in cancer cells.
    Methods: Synthesized compounds were purified by column chromatography. The MDR modulation of ABCB1 was determined in cellular efflux assays using the flow cytometry technique and cellular fluorescent measurements by the use of each fluorescent substrate.
    Results: Compounds were yielded in a two-step reaction with structurally varied components. Further, substituent- dependent effects on the determined MDR inhibiting properties towards ABCB1 were discussed. Cellular studies prove that there is no toxicity or restoration of cancer cell sensitivity towards the used anticancer drug.
    Conclusion: Novel MDR modulators could be identified with favorable methoxy and ester group functions. Their use in both ABCB1 non-expressing and overexpressing cells proves a selective toxicity-increasing effect of the applied anticancer agent in the ABCB1 overexpressing cells, whereas the toxicity effect of the anticancer drug was almost unchanged in the non-expressing cells. These results qualify our novel compounds as perspective anticancer drugs compared to MDR modulators with nonselective toxicity properties.
    Language English
    Publishing date 2024-05-03
    Publishing country Netherlands
    Document type Journal Article
    ZDB-ID 2217610-X
    ISSN 1875-5992 ; 1871-5206
    ISSN (online) 1875-5992
    ISSN 1871-5206
    DOI 10.2174/0118715206314406240502054139
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Zs.A 5583: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (2.OG)
    ab Jg. 2022: Lesesaal (EG)

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  4. Article ; Online: Synthesis and Antibacterial Evaluation of Novel Small-Molecule Antibacterials of a Reduced Acridine Structure in S. aureus Strains Including MRSA.

    Werner, Peter / Kreutzer, David / Szemeredi, Nikoletta / Spengler, Gabriella / Hilgeroth, Andreas

    Medicinal chemistry (Shariqah (United Arab Emirates))

    2024  

    Abstract: Background: The increasing antibacterial drug resistance remains a threat to global health with increasing mortality and morbidity. There is an urgent need to find novel antibacterials and develop alternative strategies to combat the increasing ... ...

    Abstract Background: The increasing antibacterial drug resistance remains a threat to global health with increasing mortality and morbidity. There is an urgent need to find novel antibacterials and develop alternative strategies to combat the increasing antibacterial drug resistance.

    Objective: We aimed to synthesize novel small-molecule antibacterials to evaluate the structuredependent antibacterial compound activities against S. aureus and MRSA.

    Method: Compounds were synthesized by primary N-alkylation to form alkyl acridinium salts that were further functionalized with substituted phenyl residues and finally purified by column chromatography. The antibacterial growth inhibition activity was determined as MIC value.

    Results: The substituent effects on the determined antibacterial growth inhibitory properties have been discussed.

    Conclusion: The best activities have been found for compounds with methoxy functions, exceeding the activities of reported novel antibacterial peptides. The compounds have also shown antibacterial drug-enhancing effects, which have been manifested as a reduction in the MIC values of the used antibiotics.
    Language English
    Publishing date 2024-05-09
    Publishing country Netherlands
    Document type Journal Article
    ISSN 1875-6638
    ISSN (online) 1875-6638
    DOI 10.2174/0115734064302048240424045239
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  5. Article ; Online: MDR Inhibitors for Anticancer Therapy.

    Werner, Peter / Hilgeroth, Andreas

    Anti-cancer agents in medicinal chemistry

    2021  Volume 22, Issue 7, Page(s) 1242–1243

    MeSH term(s) Antineoplastic Agents/pharmacology ; Antineoplastic Agents/therapeutic use ; Drug Resistance, Multiple ; Drug Resistance, Neoplasm ; Humans
    Chemical Substances Antineoplastic Agents
    Language English
    Publishing date 2021-10-13
    Publishing country Netherlands
    Document type Journal Article
    ZDB-ID 2217610-X
    ISSN 1875-5992 ; 1871-5206
    ISSN (online) 1875-5992
    ISSN 1871-5206
    DOI 10.2174/1871520621666210922112404
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 5583: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (2.OG)
    ab Jg. 2022: Lesesaal (EG)

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  6. Article ; Online: Correction: Döring et al. Discovery of Novel Symmetrical 1,4-Dihydropyridines as Inhibitors of Multidrug-Resistant Protein (MRP4) Efflux Pump for Anticancer Therapy.

    Döring, Henry / Kreutzer, David / Ritter, Christoph / Hilgeroth, Andreas

    Molecules (Basel, Switzerland)

    2022  Volume 27, Issue 11

    Abstract: The authors would like to correct an error made through no fault of their own in the title paper [ ... ]. ...

    Abstract The authors would like to correct an error made through no fault of their own in the title paper [...].
    Language English
    Publishing date 2022-06-02
    Publishing country Switzerland
    Document type Published Erratum
    ZDB-ID 1413402-0
    ISSN 1420-3049 ; 1431-5165 ; 1420-3049
    ISSN (online) 1420-3049
    ISSN 1431-5165 ; 1420-3049
    DOI 10.3390/molecules27113575
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.MO 81: Show issues

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  7. Article ; Online: Synthesis and Evaluation of Novel Substituted N-Aryl 1,4-Dihydropyridines as Antituberculostatic Agents.

    Seitz, Lisa / Reiling, Norbert / Vorreiter, Christopher / Sippl, Wolfgang / Kessler, Sonja / Hilgeroth, Andreas

    Medicinal chemistry (Shariqah (United Arab Emirates))

    2023  Volume 20, Issue 1, Page(s) 30–39

    Abstract: Background: Tuberculosis has been the main cause of mortality of infectious diseases worldwide, with strongly limited therapeutic options. With increasing resistance and missing suitable drugs in those cases, there is a strong need for novel ... ...

    Abstract Background: Tuberculosis has been the main cause of mortality of infectious diseases worldwide, with strongly limited therapeutic options. With increasing resistance and missing suitable drugs in those cases, there is a strong need for novel antituberculostatic drugs. We developed novel N-aryl 1,4-dihydropyridines with various substitution patterns to evaluate them as antituberculostatic agents.
    Methods: 1,4-Dihydropyridine derivatives were synthesized and purified by column chromatography or recrystallization. The mycobacterial growth inhibition was determined in a fluorescent mycobacterial growth assay.
    Results: The compounds were prepared in a simple one-pot reaction under acidic conditions with structurally varied components. The substituent effects on the determined mycobacterial growth inhibitory properties are discussed.
    Conclusion: Lipophilic diester substituted derivatives show promising activities that were additionally affected by the aromatic substituent functions. Thus, we identified compounds with activities almost reaching that of the used antimycobacterial drug as control.
    MeSH term(s) Antitubercular Agents ; Mycobacterium tuberculosis ; Structure-Activity Relationship ; Dihydropyridines ; Microbial Sensitivity Tests
    Chemical Substances Antitubercular Agents ; Dihydropyridines
    Language English
    Publishing date 2023-06-23
    Publishing country Netherlands
    Document type Journal Article
    ISSN 1875-6638
    ISSN (online) 1875-6638
    DOI 10.2174/1573406419666230622121512
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  8. Article: Novel Nonsymmetrical 1,4-Dihydropyridines as Inhibitors of Nonsymmetrical MRP-Efflux Pumps for Anticancer Therapy.

    Kreutzer, David / Ritter, Christoph A / Hilgeroth, Andreas

    Pharmaceuticals (Basel, Switzerland)

    2020  Volume 13, Issue 7

    Abstract: Cancer is a strong global burden with increasing numbers of diseases and ongoing anticancer drug resistance. The number of structurally novel anticancer drugs is strongly limited. They cause high costs for the social health systems. Most critical so- ... ...

    Abstract Cancer is a strong global burden with increasing numbers of diseases and ongoing anticancer drug resistance. The number of structurally novel anticancer drugs is strongly limited. They cause high costs for the social health systems. Most critical so-called multidrug resistances (MDR) are caused by transmembrane efflux pumps that transport drugs with various structures out of the cancer cells. Multidrug resistance proteins (MRPs) type 1 and 2 are found overexpressed in various kinds of cancer. There is a strong need for inhibitors of those efflux pumps. We developed novel nonsymmetrical 1,4-dihydropyridines as novel inhibitors of cancer relevant MRP types 1 and 2. The structure-dependent activities of the differently substituted derivatives were evaluated in cellular assays of respective cancer cells and are discussed. Promising candidates were identified. One candidate was demonstrated to resensitize a cisplatin resistant cancer cell line and thus to overcome the anticancer drug resistance.
    Language English
    Publishing date 2020-07-09
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2193542-7
    ISSN 1424-8247
    ISSN 1424-8247
    DOI 10.3390/ph13070146
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  9. Article ; Online: Discovery of Novel Symmetrical 1,4-Dihydropyridines as Inhibitors of Multidrug-Resistant Protein (MRP4) Efflux Pump for Anticancer Therapy.

    Döring, Henry / Kreutzer, David / Ritter, Christoph / Hilgeroth, Andreas

    Molecules (Basel, Switzerland)

    2020  Volume 26, Issue 1

    Abstract: Despite the development of targeted therapies in cancer, the problem of multidrug resistance (MDR) is still unsolved. Most patients with metastatic cancer die from MDR. Transmembrane efflux pumps as the main cause of MDR have been addressed by developed ... ...

    Abstract Despite the development of targeted therapies in cancer, the problem of multidrug resistance (MDR) is still unsolved. Most patients with metastatic cancer die from MDR. Transmembrane efflux pumps as the main cause of MDR have been addressed by developed inhibitors, but early inhibitors of the most prominent and longest known efflux pump P-glycoprotein (P-gp) were disappointing. Those inhibitors have been used without knowledge about the expression of P-gp by the treated tumor. Therefore the use of inhibitors of transmembrane efflux pumps in clinical settings is reconsidered as a promising strategy in the case of the respective efflux pump expression. We discovered novel symmetric inhibitors of the symmetric efflux pump MRP4 encoded by the ABCC4 gene. MRP4 is involved in many kinds of cancer with resistance to anticancer drugs. All compounds showed better activities than the best known MRP4 inhibitor MK571 in an MRP4-overexpressing cell line assay, and the activities could be related to the various substitution patterns of aromatic residues within the symmetric molecular framework. One of the best compounds was demonstrated to overcome the MRP4-mediated resistance in the cell line model to restore the anticancer drug sensitivity as a proof of concept.
    MeSH term(s) Antineoplastic Agents/chemistry ; Antineoplastic Agents/pharmacology ; Cell Line, Tumor ; Dihydropyridines/chemistry ; Dihydropyridines/pharmacology ; Drug Discovery/methods ; Drug Resistance, Multiple/drug effects ; Drug Resistance, Neoplasm/drug effects ; Drug Screening Assays, Antitumor/methods ; Humans ; Magnetic Resonance Spectroscopy ; Multidrug Resistance-Associated Proteins/antagonists & inhibitors ; Multidrug Resistance-Associated Proteins/chemistry
    Chemical Substances ABCC4 protein, human ; Antineoplastic Agents ; Dihydropyridines ; Multidrug Resistance-Associated Proteins
    Language English
    Publishing date 2020-12-22
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 1413402-0
    ISSN 1420-3049 ; 1431-5165 ; 1420-3049
    ISSN (online) 1420-3049
    ISSN 1431-5165 ; 1420-3049
    DOI 10.3390/molecules26010018
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.MO 81: Show issues

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  10. Article: Novel Effective Fluorinated Benzothiophene-Indole Hybrid Antibacterials against

    Seethaler, Marius / Hertlein, Tobias / Hopke, Elisa / Köhling, Paul / Ohlsen, Knut / Lalk, Michael / Hilgeroth, Andreas

    Pharmaceuticals (Basel, Switzerland)

    2022  Volume 15, Issue 9

    Abstract: Increasing antibacterial drug resistance threatens global health, unfortunately, however, efforts to find novel antibacterial agents have been scaled back by the pharmaceutical industry due to concerns about a poor return on investment. Nevertheless, ... ...

    Abstract Increasing antibacterial drug resistance threatens global health, unfortunately, however, efforts to find novel antibacterial agents have been scaled back by the pharmaceutical industry due to concerns about a poor return on investment. Nevertheless, there is an urgent need to find novel antibacterial compounds to combat antibacterial drug resistance. The synthesis of novel drugs from natural sources is mostly cost-intensive due to those drugs' complicated structures. Therefore, it is necessary to find novel antibacterials by simple synthesis to become more attractive for industrial production. We succeeded in the discovery of four antibacterial compound (sub)classes accessible in a simple one-pot reaction based on fluorinated benzothiophene-indole hybrids. They have been evaluated against various
    Language English
    Publishing date 2022-09-13
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2193542-7
    ISSN 1424-8247
    ISSN 1424-8247
    DOI 10.3390/ph15091138
    Database MEDical Literature Analysis and Retrieval System OnLINE

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