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Issue 4, 2015
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Pyrrole- and indole-containing tranylcypromine derivatives as novel lysine-specific demethylase 1 inhibitors active on cancer cells

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Abstract

On the basis of previous research showing the capability of N-carbobenzyloxy-(Z-)amino acid-tranylcypromine (-TCPA) derivatives to inhibit LSD1, we inserted at the 4-amino-TCPA moiety first a Z-Pro (9) and a Z-Gly (10) residue and then, after the encouraging data obtained for 9, a pyrrole and an indole ring in which the relative N1 position carried a acetophenone, a N-phenyl/benzylacetamide, or a Z chain (11a–f and 12a–f, respectively). In both series, the Z-pyrrole and indole derivatives 11e, f and 12e, f displayed high LSD1 inhibitory activity. The compounds are able to inhibit LSD1 in NB4 cells, increasing the expression of two related genes, GFI-1b and ITGAM, and to induce cell growth arrest in the AML MB4-11 and APL NB4 cell lines.

Graphical abstract: Pyrrole- and indole-containing tranylcypromine derivatives as novel lysine-specific demethylase 1 inhibitors active on cancer cells

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Supplementary files

Article information


Submitted
08 Nov 2014
Accepted
19 Dec 2014
First published
23 Dec 2014

Med. Chem. Commun., 2015,6, 665-670
Article type
Concise Article
Author version available

Pyrrole- and indole-containing tranylcypromine derivatives as novel lysine-specific demethylase 1 inhibitors active on cancer cells

V. Rodriguez, S. Valente, S. Rovida, D. Rotili, G. Stazi, A. Lucidi, G. Ciossani, A. Mattevi, O. A. Botrugno, P. Dessanti, C. Mercurio, P. Vianello, S. Minucci, M. Varasi and A. Mai, Med. Chem. Commun., 2015, 6, 665
DOI: 10.1039/C4MD00507D

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