TY - JOUR
T1 - Pyrrole- and indole-containing tranylcypromine derivatives as novel lysine-specific demethylase 1 inhibitors active on cancer cells
AU - Rodriguez, Veronica
AU - Valente, Sergio
AU - Rovida, Stefano
AU - Rotili, Dante
AU - Stazi, Giulia
AU - Lucidi, Alessia
AU - Ciossani, Giuseppe
AU - Mattevi, Andrea
AU - Botrugno, Oronza A.
AU - Dessanti, Paola
AU - Mercurio, Ciro
AU - Vianello, Paola
AU - Minucci, Saverio
AU - Varasi, Mario
AU - Mai, Antonello
PY - 2015/4/1
Y1 - 2015/4/1
N2 - 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. This journal is
AB - 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. This journal is
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U2 - 10.1039/c4md00507d
DO - 10.1039/c4md00507d
M3 - Article
AN - SCOPUS:84928004801
VL - 6
SP - 665
EP - 670
JO - MedChemComm
JF - MedChemComm
SN - 2040-2503
IS - 4
ER -