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

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

Content Provider	World Health Organization (WHO)-Global Index Medicus
Author	Han, Yan Wu, Chunlei Lv, Haifeng Liu, Na Deng, Huaying
Description	Author Affiliation: Han Y ( Department of Orthopedics, The First Affiliated Hospital, Wenzhou Medical University.)
Abstract	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.
File Format	HTM / HTML
ISSN	00092363
e-ISSN	13475223
Journal	Chemical and Pharmaceutical Bulletin
Issue Number	11
Volume Number	63
Language	English
Publisher	The Pharmaceutical Society of Japan
Publisher Date	2015-01-01
Publisher Place	Japan
Access Restriction	Open
Subject Keyword	Discipline Pharmacology Antineoplastic Agents Chemistry Pharmacology Histone Demethylases Antagonists & Inhibitors Tranylcypromine Analogs & Derivatives Cell Line, Tumor Cell Proliferation Drug Effects Coumaric Acids Metabolism Monoamine Oxidase Inhibitors Neoplasms Drug Therapy Enzymology Pathology Structure-activity Relationship
Content Type	Text
Resource Type	Article
Subject	Chemistry Medicine Drug Discovery

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