Synthesis, Pim kinase inhibitory potencies and in vitro antiproliferative activities of diversely substituted pyrrolo[2,3-a]carbazoles

Rufine Akue-Gedu, Lionel Nauton, Vincent Thery, Jenny Bain, Philip Cohen, Fabrice Anizon, Pascale Moreau

    Research output: Contribution to journalArticle

    28 Citations (Scopus)

    Abstract

    The synthesis of new pyrrolo[2,3-a]carbazole derivatives diversely substituted at the C-6 to C-9 positions is described. These compounds were tested for their kinase inhibitory potencies toward three kinases (Pim-1, Pim-2, Pim-3) as well as for their in vitro antiproliferative activities toward a human fibroblast primary culture and three human solid cancer cell lines (PC3, DU145, and PA 1). Moreover, molecular docking studies were performed to explain the enhanced inhibitory activity of the most active compound 3d. (C) 2010 Elsevier Ltd. All rights reserved.

    Original languageEnglish
    Pages (from-to)6865-6873
    Number of pages9
    JournalBioorganic & Medicinal Chemistry
    Volume18
    Issue number18
    DOIs
    Publication statusPublished - 15 Sep 2010

    Keywords

    • Pyrrolo[2,3-a]carbazoles
    • Kinase inhibitors
    • PIM inhibitors, In vitro antiproliferative activities
    • SPECIFICITY
    • DOCKING

    Cite this

    Akue-Gedu, Rufine ; Nauton, Lionel ; Thery, Vincent ; Bain, Jenny ; Cohen, Philip ; Anizon, Fabrice ; Moreau, Pascale. / Synthesis, Pim kinase inhibitory potencies and in vitro antiproliferative activities of diversely substituted pyrrolo[2,3-a]carbazoles. In: Bioorganic & Medicinal Chemistry. 2010 ; Vol. 18, No. 18. pp. 6865-6873.
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    abstract = "The synthesis of new pyrrolo[2,3-a]carbazole derivatives diversely substituted at the C-6 to C-9 positions is described. These compounds were tested for their kinase inhibitory potencies toward three kinases (Pim-1, Pim-2, Pim-3) as well as for their in vitro antiproliferative activities toward a human fibroblast primary culture and three human solid cancer cell lines (PC3, DU145, and PA 1). Moreover, molecular docking studies were performed to explain the enhanced inhibitory activity of the most active compound 3d. (C) 2010 Elsevier Ltd. All rights reserved.",
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    Synthesis, Pim kinase inhibitory potencies and in vitro antiproliferative activities of diversely substituted pyrrolo[2,3-a]carbazoles. / Akue-Gedu, Rufine; Nauton, Lionel; Thery, Vincent; Bain, Jenny; Cohen, Philip; Anizon, Fabrice; Moreau, Pascale.

    In: Bioorganic & Medicinal Chemistry, Vol. 18, No. 18, 15.09.2010, p. 6865-6873.

    Research output: Contribution to journalArticle

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    T1 - Synthesis, Pim kinase inhibitory potencies and in vitro antiproliferative activities of diversely substituted pyrrolo[2,3-a]carbazoles

    AU - Akue-Gedu, Rufine

    AU - Nauton, Lionel

    AU - Thery, Vincent

    AU - Bain, Jenny

    AU - Cohen, Philip

    AU - Anizon, Fabrice

    AU - Moreau, Pascale

    PY - 2010/9/15

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    AB - The synthesis of new pyrrolo[2,3-a]carbazole derivatives diversely substituted at the C-6 to C-9 positions is described. These compounds were tested for their kinase inhibitory potencies toward three kinases (Pim-1, Pim-2, Pim-3) as well as for their in vitro antiproliferative activities toward a human fibroblast primary culture and three human solid cancer cell lines (PC3, DU145, and PA 1). Moreover, molecular docking studies were performed to explain the enhanced inhibitory activity of the most active compound 3d. (C) 2010 Elsevier Ltd. All rights reserved.

    KW - Pyrrolo[2,3-a]carbazoles

    KW - Kinase inhibitors

    KW - PIM inhibitors, In vitro antiproliferative activities

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    KW - DOCKING

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    JO - Bioorganic & Medicinal Chemistry

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