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  1. Article ; Online: Anti-Inflammatory Effects of a Novel Nuclear Factor-

    Baba, Hiroyuki / Hosoya, Tadashi / Ishida, Ryosuke / Tai, Kenpei / Hatsuzawa, Saki / Kondo, Yuma / Kusuhara, Hiroyuki / Kagechika, Hiroyuki / Yasuda, Shinsuke

    The Journal of pharmacology and experimental therapeutics

    2024  Volume 388, Issue 3, Page(s) 788–797

    Abstract: Nuclear factor- ...

    Abstract Nuclear factor-
    MeSH term(s) Mice ; Animals ; NF-kappa B/metabolism ; Arthritis, Experimental/pathology ; Chromatography, Liquid ; Tandem Mass Spectrometry ; Inflammation/drug therapy ; Anti-Inflammatory Agents/pharmacology ; Anti-Inflammatory Agents/therapeutic use ; Hepatitis/drug therapy ; Pyrimidines/adverse effects ; Inflammation Mediators/metabolism ; Amines/therapeutic use ; Immunoglobulin G
    Chemical Substances NF-kappa B ; Anti-Inflammatory Agents ; Pyrimidines ; Inflammation Mediators ; Amines ; Immunoglobulin G
    Language English
    Publishing date 2024-02-15
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 3106-9
    ISSN 1521-0103 ; 0022-3565
    ISSN (online) 1521-0103
    ISSN 0022-3565
    DOI 10.1124/jpet.123.001904
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: Comprehensive exploration of chemical space using trisubstituted carboranes.

    Asawa, Yasunobu / Hatsuzawa, Saki / Yoshimori, Atsushi / Yamada, Kentaro / Katoh, Akira / Kouji, Hiroyuki / Nakamura, Hiroyuki

    Scientific reports

    2021  Volume 11, Issue 1, Page(s) 24101

    Abstract: A total of 42 trisubstituted carboranes categorised into five scaffolds were systematically designed and synthesized by exploiting the different reactivities of the twelve vertices of o-, m-, and p-carboranes to cover all directions in chemical space. ... ...

    Abstract A total of 42 trisubstituted carboranes categorised into five scaffolds were systematically designed and synthesized by exploiting the different reactivities of the twelve vertices of o-, m-, and p-carboranes to cover all directions in chemical space. Significant inhibitors of hypoxia inducible factor transcriptional activitay were mainly observed among scaffold V compounds (e.g., Vi-m, and Vo), whereas anti-rabies virus activity was observed among scaffold V (Va-h), scaffold II (IIb-g), and scaffold IV (IVb) compounds. The pharmacophore model predicted from compounds with scaffold V, which exhibited significant anti-rabies virus activity, agreed well with compounds IIb-g with scaffold II and compound IVb with scaffold IV. Normalized principal moment of inertia analysis indicated that carboranes with scaffolds I-V cover all regions in the chemical space. Furthermore, the first compounds shown to stimulate the proliferation of the rabies virus were found among scaffold V carboranes.
    Language English
    Publishing date 2021-12-16
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2615211-3
    ISSN 2045-2322 ; 2045-2322
    ISSN (online) 2045-2322
    ISSN 2045-2322
    DOI 10.1038/s41598-021-03459-6
    Database MEDical Literature Analysis and Retrieval System OnLINE

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