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  • 1
    Online Resource
    Online Resource
    Recent progress of research on anti‐tumor agents using benzimidazole as the structure unit
    Wiley ; 2022
    In:  Chemical Biology & Drug Design Vol. 99, No. 5 ( 2022-05), p. 736-757
    Details
    In: Chemical Biology & Drug Design, Wiley, Vol. 99, No. 5 ( 2022-05), p. 736-757
    Abstract: With the development of exploration for disease‐related proteins or receptors, more and more novel structural lead compounds are required to designed and synthesized. The benzimidazole is an effective structural unit in which the benzene ring is fused at the 4 and 5 positions of the imidazole ring and wildly used in drug design. Here, we introduce some recent progress of research for anti‐tumor agents which was target to various target proteins such as DNA topoisomerase, angiogenesis, serine/threonine protein kinase, and tyrosine protein kinase. These anti‐tumor agents are all introduced benzimidazole as the structure unit. Further docking study showed that the benzimidazole group was not only act as a skeleton to expand the structure of molecule but also as an excellent ligand unit to form hydrogen bond or π–π conjugation and hydrophobic interaction with target proteins or receptors. We expect that introducing benzimidazole in the chemical structure could be a reasonable and priority strategy in novel anti‐tumor agents' design.
    Type of Medium: Online Resource
    ISSN: 1747-0277 , 1747-0285
    URL: Issue
    URL: Article
    DOI: 10.1111/cbdd.v99.5
    DOI: 10.1111/cbdd.14022
    Language: English
    Publisher: Wiley
    Publication Date: 2022
    detail.hit.zdb_id: 2216600-2
    SSG: 12
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  • 2
    Online Resource
    Online Resource
    Recent Progress in the Research on Benzimidazole PARP-1 Inhibitors
    Bentham Science Publishers Ltd. ; 2022
    In:  Mini-Reviews in Medicinal Chemistry Vol. 22, No. 19 ( 2022-10), p. 2438-2462
    Details
    In: Mini-Reviews in Medicinal Chemistry, Bentham Science Publishers Ltd., Vol. 22, No. 19 ( 2022-10), p. 2438-2462
    Abstract: Poly (ADP-ribose) polymerase-1 (PARP-1) is a multifunctional protein that plays an important role in DNA repair and genome integrity. PARP-1 inhibitors can be used as effective drugs not only to treat BRCA-1/2 deficient cancers because of the synthetic lethality effect but also to treat non- BRCA1/2 deficient tumours because of the effect of PARP capture. Therefore, PARP inhibitors have become a focus of compelling research. Among these inhibitors, substituted benzimidazole derivatives were mainly concerned as lead compounds. However, the commercially available benzimidazole PARP-1 inhibitors have some shortcomings, such as serious toxicity in combination with chemotherapy drugs and in vivo cardiovascular side effects such as anemia. Therefore it is crucial for scientists to explore more structure-activity relationships of the benzimidazole PARP-1 inhibitors and access safer and more effective PARP inhibitors. As the binding regions of PARP-1 and the substrates are usually characterized by NI site and AD site, the modification of benzimidazoles mainly occurs on the benzimidazole skeleton (NI site) and the side chain of benzimidazole in the 2-C position (AD site). Herein, the recent progress in the research on benzamides PARP inhibitors was introduced. We noticed that even though many efforts were made to the modification of NI sites, there was still a lack of optimistic and impressive results. However, the structure-activity relationships of the modification of AD sites have not been thoroughly discovered yet. We hope that enlightened by the previous research, more research on AD sites should be carried out, and more effective benzimidazole PARP-1 inhibitors could be designed, synthesized, and applied to clinics.
    Type of Medium: Online Resource
    ISSN: 1389-5575
    URL: Article
    DOI: 10.2174/1389557522666220321150700
    Language: English
    Publisher: Bentham Science Publishers Ltd.
    Publication Date: 2022
    SSG: 15,3
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  • 3
    Online Resource
    Online Resource
    Multiply quaternized poly(phenylene oxide)s bearing β-cyclodextrin pendants as “assisting moiety” for high-performance anion exchange membranes
    Elsevier BV ; 2022
    In:  Journal of Membrane Science Vol. 660 ( 2022-10), p. 120881-
    Details
    In: Journal of Membrane Science, Elsevier BV, Vol. 660 ( 2022-10), p. 120881-
    Type of Medium: Online Resource
    ISSN: 0376-7388
    URL: Article
    DOI: 10.1016/j.memsci.2022.120881
    Language: English
    Publisher: Elsevier BV
    Publication Date: 2022
    detail.hit.zdb_id: 1491419-0
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  • 4
    Online Resource
    Online Resource
    Fabrication of Cross‐Linked Anion Exchange Membranes Using a Pillar[5]arene Bearing Multiple Alkyl Bromide Head Groups as Cross‐Linker
    Wiley ; 2020
    In:  Macromolecular Materials and Engineering Vol. 305, No. 7 ( 2020-07)
    Details
    In: Macromolecular Materials and Engineering, Wiley, Vol. 305, No. 7 ( 2020-07)
    Abstract: A pillararene‐based macrocycle with up to 10 flexible chains bearing alkyl bromide head groups is synthesized and investigated for the first time as a multiarm cross‐linker for tertiary‐amine functionalized polyethersulfone. Different from any previously reported cross‐linker, this has a unique pillar‐shaped structure and abundant reactive sites to form multifunctional clusters in the conductive domain. This advantage enables cross‐linking to occur smoothly at the membrane‐casting stage and endows the cross‐linked membranes with improved performance. The cross‐linked anion exchange membranes are found to possess high conductivities and excellent alkaline stability. With a controllable swelling ratio of 19.5%, the maximum conductivity of a membrane can reach 155 mS cm –1 at 80 °C. Due to its local high‐density cross‐linked structure, a delay in degradation kinetics under alkaline condition can be observed, and the loss of conductivity is 〈 10% after 400 h of alkaline stability test at 80 °C.
    Type of Medium: Online Resource
    ISSN: 1438-7492 , 1439-2054
    URL: Issue
    URL: Article
    DOI: 10.1002/mame.v305.7
    DOI: 10.1002/mame.202000158
    Language: English
    Publisher: Wiley
    Publication Date: 2020
    detail.hit.zdb_id: 2004372-7
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  • 5
    Online Resource
    Online Resource
    Design, synthesis, and evaluation of 1 H ‐benzo[d]imidazole‐4‐carboxamide PARP ‐1 inhibitors using different saturated nitrogen‐contained heterocycle as linker group
    Wiley ; 2023
    In:  Chemical Biology & Drug Design Vol. 101, No. 6 ( 2023-06), p. 1335-1347
    Details
    In: Chemical Biology & Drug Design, Wiley, Vol. 101, No. 6 ( 2023-06), p. 1335-1347
    Abstract: Poly (ADP‐ribose) polymerase‐1 (PARP‐1) inhibitors have been successfully applied in the clinical treatment of various cancer. Side effects and drug resistant cases were reported, and more effective PARP‐1 inhibitors were required. However, studies on the AD site of PARP‐1 inhibitors are currently incomplete. Therefore, to synthesize more potential candidate PARP‐1 inhibitors and disclose some AD site SAR of the PARP‐1 inhibitors, herein, a series of 2‐phenyl‐benzimidazole‐4‐carboxamide derivatives using different saturated nitrogen‐contained heterocycles as linker group ( 6a‐6t ) have been designed, synthesized, and evaluated PARP‐1 inhibitory activity and proliferation inhibitory against BRCA‐1 mutant MDA‐MB‐436 cell line in vitro. The results showed 6b (IC50 = 8.65 nM) exhibited the most PARP‐1 enzyme inhibitory activity comparable with Veliparib (IC50 = 15.54 nM) and Olaparib (IC50 = 2.77 nM); 6m exhibited the strongest MDA‐MB‐436 cell anti‐proliferation activity (IC50 = 25.36 ± 6.06 μM) comparable with Olaparib (IC50 = 23.89 ± 3.81 μM). The compounds 6b , 6r , and 6m could be potential candidates for effective PARP‐1 inhibitors and valuable for further optimization. The analysis of activity data also showed that the holistically anti‐proliferation activity of the 1,4‐diazepane group was about~twofold than that of the piperazine group. Meanwhile, the terminal 3‐methyl‐furanyl group exhibited the most robust PARP‐1 inhibitory and anti‐proliferation activity. It is hoped that the results could benefitable for further optimization of PARP‐1 inhibitors. Furthermore, we note that some compounds ( 6d , 6g , 6n , 6p , 6s ) showed poor PARP‐1 inhibitory ( 〉 500 nM) but relatively good anti‐proliferation activity, which indicates the proliferation inhibitory mechanism against MDA‐MB‐436 cell line was worth investigating in‐depth.
    Type of Medium: Online Resource
    ISSN: 1747-0277 , 1747-0285
    URL: Issue
    URL: Article
    DOI: 10.1111/cbdd.v101.6
    DOI: 10.1111/cbdd.14216
    Language: English
    Publisher: Wiley
    Publication Date: 2023
    detail.hit.zdb_id: 2216600-2
    SSG: 12
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  • 6
    Online Resource
    Online Resource
    Image_1.jpg
    Frontiers Media SA ; 2022
    In:  Frontiers in Immunology Vol. 13 ( 2022-11-29)
    Details
    In: Frontiers in Immunology, Frontiers Media SA, Vol. 13 ( 2022-11-29)
    Abstract: Gliomas, originating from the glial cells, are the most lethal type of primary tumors in the central nervous system. Standard treatments like surgery have not significantly improved the prognosis of glioblastoma patients. Recently, immune therapy has become a novel and effective option. As a conserved group of transcriptional regulators, the Sry-type HMG box (SOX) family has been proved to have a correlation with numerous diseases. Based on the large-scale machine learning, we found that the SOX family, with significant immune characteristics and genomic profiles, can be divided into two distinct clusters in gliomas, among which SOX10 was identified as an excellent immune regulator of macrophage in gliomas. The high expression of SOX10 is related to a shorter OS in LGG, HGG, and pan-cancer groups but benefited from the immunotherapy. It turned out in single-cell sequencing that SOX10 is high in neurons, M1 macrophages, and neural stem cells. Also, macrophages are found to be elevated in the SOX10 high-expression group. SOX10 has a positive correlation with macrophage cytokine production and negative regulation of macrophages’ chemotaxis and migration. In conclusion, our study demonstrates the outstanding cluster ability of the SOX family, indicating that SOX10 is an immune regulator of macrophage in gliomas, which can be an effective target for glioma immunotherapy.
    Type of Medium: Online Resource
    ISSN: 1664-3224
    URL: Article
    URL: Article
    DOI: 10.3389/fimmu.2022.1007461
    DOI: 10.3389/fimmu.2022.1007461.s001
    Language: Unknown
    Publisher: Frontiers Media SA
    Publication Date: 2022
    detail.hit.zdb_id: 2606827-8
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  • 7
    Online Resource
    Online Resource
    DataSheet_2.doc
    Frontiers Media SA ; 2022
    In:  Frontiers in Immunology Vol. 13 ( 2022-12-22)
    Details
    In: Frontiers in Immunology, Frontiers Media SA, Vol. 13 ( 2022-12-22)
    Abstract: CD161 has been linked to the appearance and development of various cancers. Methods The mutation map and the variation of CNVs and SNVs of CD161 were displayed according to cBioportal and GSCALite. We also evaluated the pathway enrichment and drug sensitivity of CD161 according to GSCALite. We performed a single-cell sequencing analysis of cancer cells and T cells in melanoma. The cell communication patterns related to CD161 were further explored. Multiplex immunofluorescence staining of tissue microarrays was used to detect the association between CD161 expression and macrophages and T cells. Results A high CD161 level was related to neoantigens expression, pathway enrichment, and drug sensitivity. In addition, single-cell sequencing analysis showed that CD161 was mainly expressed in T cells, M1 and M2 Macrophages, neoplastic, microglial cells, neurons, and cancer cells in many tumor types. Further study on pseudotime trajectories and functional annotation of CD161 proved the critical role of CD161 in tumor progression and T cell immunity in melanoma. Multiplex immunofluorescence revealed that CD161 is closely correlated with the immune infiltration of T cells and macrophages in multiple cancers. In addition, high CD161 expression predicted a favorable immunotherapy response. Conclusion CD161 is involved in the immune infiltration of T cells and macrophages and might be a promising target for tumor immunotherapy.
    Type of Medium: Online Resource
    ISSN: 1664-3224
    URL: Article
    URL: Article
    URL: Article
    DOI: 10.3389/fimmu.2022.1040289
    DOI: 10.3389/fimmu.2022.1040289.s001
    DOI: 10.3389/fimmu.2022.1040289.s002
    Language: Unknown
    Publisher: Frontiers Media SA
    Publication Date: 2022
    detail.hit.zdb_id: 2606827-8
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  • 8
    Online Resource
    Online Resource
    High affinity and low PARP-trapping benzimidazole derivatives as a potential warhead for PARP1 degraders
    Elsevier BV ; 2024
    In:  European Journal of Medicinal Chemistry Vol. 271 ( 2024-05), p. 116405-
    Details
    In: European Journal of Medicinal Chemistry, Elsevier BV, Vol. 271 ( 2024-05), p. 116405-
    Type of Medium: Online Resource
    ISSN: 0223-5234
    URL: Article
    DOI: 10.1016/j.ejmech.2024.116405
    Language: English
    Publisher: Elsevier BV
    Publication Date: 2024
    detail.hit.zdb_id: 2005170-0
    SSG: 15,3
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  • 9
    Online Resource
    Online Resource
    Interfacial Approach toward Benzene‐Bridged Polypyrrole Film–Based Micro‐Supercapacitors with Ultrahigh Volumetric Power Density
    Wiley ; 2020
    In:  Advanced Functional Materials Vol. 30, No. 7 ( 2020-02)
    Details
    In: Advanced Functional Materials, Wiley, Vol. 30, No. 7 ( 2020-02)
    Abstract: 2D soft nanomaterials are an emerging research field due to their versatile chemical structures, easily tunable properties, and broad application potential. In this study, a benzene‐bridged polypyrrole film with a large area, up to a few square centimeters, is synthesized through an interfacial polymerization approach. As‐prepared semiconductive films exhibit a bandgap of ≈2 eV and a carrier mobility of ≈1.5 cm 2 V −1 s −1 , inferred from time‐resolved terahertz spectroscopy. The samples are employed to fabricate in‐plane micro‐supercapacitors (MSCs) by laser scribing and exhibit an ultrahigh areal capacitance of 0.95 mF cm −2 , using 1‐ethyl‐3‐methylimidazolium tetrafluoroborate ([EMIM][BF 4 ]) as an electrolyte. Importantly, the maximum energy and power densities of the developed MSCs reach values up to 50.7 mWh cm −3 and 9.6 kW cm −3 , respectively; the performance surpassing most of the 2D material‐based MSCs is reported to date.
    Type of Medium: Online Resource
    ISSN: 1616-301X , 1616-3028
    URL: Issue
    URL: Article
    DOI: 10.1002/adfm.v30.7
    DOI: 10.1002/adfm.201908243
    Language: English
    Publisher: Wiley
    Publication Date: 2020
    detail.hit.zdb_id: 2029061-5
    detail.hit.zdb_id: 2039420-2
    SSG: 11
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  • 10
    Online Resource
    Online Resource
    Synthesis and evaluation of 2‐(4‐[4‐acetylpiperazine‐1‐carbonyl] phenyl)‐ 1H ‐benzo[d]imidazole‐4‐carboxamide derivatives as potential PARP ‐1 inhibitors and preliminary study on structure‐activity relationship
    Wiley ; 2022
    In:  Drug Development Research Vol. 83, No. 1 ( 2022-02), p. 55-63
    Details
    In: Drug Development Research, Wiley, Vol. 83, No. 1 ( 2022-02), p. 55-63
    Abstract: Although 1H‐benzo[d]imidazole‐4‐carboxamide derivatives have been explored for a long time, the structure–activity relationship of the substituents in the hydrophobic pocket (AD binding sites) has not thoroughly discovered. Here in, a series of 2‐(4‐[4‐acetylpiperazine‐1‐carbonyl] phenyl)‐1H‐benzo[d]imidazole‐4‐carboxamide derivatives have been designed, synthesized, and successful characterization as novel and effective poly ADP‐ribose polymerases (PARP)‐1 inhibitors to improve the structure–activity relationships about the substituents in the hydrophobic pocket. These derivatives were evaluated for their PARP‐1 inhibitory activity and cellular inhibitory against BRCA‐1 deficient cells (MDA‐MB‐436) and wild cells (MCF‐7) using PARP kit assay and MTT method. The results indicated that compared with other heterocyclic compounds, furan ring‐substituted derivatives 14n‐14q showed better PARP‐1 inhibitory activity. Among this derivatives, compound 14p displayed the strongest inhibitory effects on PARP‐1 enzyme (IC 50  = 0.023 μM), which was close to that of Olaparib. 14p (IC 50  = 43.56 ± 0.69 μM) and 14q (IC 50  = 36.69 ± 0.83 μM) displayed good antiproliferation activity on MDA‐MB‐436 cells and inactivity on MCF‐7 cells, indicating that 14p and 14q have high selectivity and targeting. The molecular docking method was used to explore the binding mode of compound 14p and PARP‐1, and implied that the formation of hydrogen bond was essential for PARP‐1 inhibition activities. This study also showed that in the hydrophobic pocket (AD binding sites), the introduction of strong electronegative groups (furan ring, e.g.) or halogen atoms in the side chain of benzimidazole might improve its inhibitory activity and this strategy could be applied in further research.
    Type of Medium: Online Resource
    ISSN: 0272-4391 , 1098-2299
    URL: Issue
    URL: Article
    DOI: 10.1002/ddr.v83.1
    DOI: 10.1002/ddr.21843
    Language: English
    Publisher: Wiley
    Publication Date: 2022
    detail.hit.zdb_id: 1500191-X
    SSG: 15,3
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