Novel Tranylcypromine/Hydroxylcinnamic Acid Hybrids as Lysine-Specific Demethylase 1 Inhibitors with Potent Antitumor Activity

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  • Han Yan
    Department of Orthopedics, The First Affiliated Hospital, Wenzhou Medical University
  • Wu Chunlei
    Department of Orthopedics, The First Affiliated Hospital, Wenzhou Medical University
  • Lv Haifeng
    School of Pharmacy, Wenzhou Medical University
  • Liu Na
    Department of Traditional Medical Traumatology Orthopedics, Xi’an Honghui Hospital
  • Deng Huaying
    Department of Orthopedics, The First Affiliated Hospital, Wenzhou Medical University

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Novel tranylcypromine/hydroxylcinnamic acid hybrids 15a, b, and 19a–l were designed and synthesized by connecting tranylcypromine with hydroxylcinnamic acid, and their biological activities were evaluated. The in vitro assay of their inhibitory activities against lysine-specific demethylase 1 (LSD1) showed that most of the target compounds displayed high potency with IC50 values ranging from submicromolar to single-digit micromolar levels. In particular, compound 19l had robust, selective LSD1 inhibitory activity, which was obviously higher than the inhibitory activity against homologues monoamine oxidase-A (MAO-A) and MAO-B, respectively. Furthermore, the most potent compound 19l selectively inhibited cancer cell but not nontumor colon cell proliferation in vitro. In addition, compound 19l also dose-dependently increased the expression of H3K4me2 at the cellular level. Our findings suggest that tranylcypromine/hydroxylcinnamic acid hybrids as LSD1 inhibitors may hold great promise as therapeutic agents for the treatment of human cancers.

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