TY - JOUR
T1 - Novel histone deacetylase inhibitors induce growth arrest, apoptosis, and differentiation in sarcoma cancer stem cells
AU - Di Pompo, Gemma
AU - Salerno, Manuela
AU - Rotili, Dante
AU - Valente, Sergio
AU - Zwergel, Clemens
AU - Avnet, Sofia
AU - Lattanzi, Giovanna
AU - Baldini, Nicola
AU - Mai, Antonello
PY - 2015/5/14
Y1 - 2015/5/14
N2 - Musculoskeletal sarcomas are aggressive malignancies of bone and soft tissues often affecting children and adolescents. Histone deacetylase inhibitors (HDACi) have been proposed to counteract cancer stem cells (CSCs) in solid neoplasms. When tested in human osteosarcoma, rhabdomyosarcoma, and Ewing's sarcoma stem cells, the new HDACi MC1742 (1) and MC2625 (2) increased acetyl-H3 and acetyl-tubulin levels and inhibited CSC growth by apoptosis induction. At nontoxic doses, 1 promoted osteogenic differentiation. Further investigation with 1 will be done in preclinical sarcoma models.
AB - Musculoskeletal sarcomas are aggressive malignancies of bone and soft tissues often affecting children and adolescents. Histone deacetylase inhibitors (HDACi) have been proposed to counteract cancer stem cells (CSCs) in solid neoplasms. When tested in human osteosarcoma, rhabdomyosarcoma, and Ewing's sarcoma stem cells, the new HDACi MC1742 (1) and MC2625 (2) increased acetyl-H3 and acetyl-tubulin levels and inhibited CSC growth by apoptosis induction. At nontoxic doses, 1 promoted osteogenic differentiation. Further investigation with 1 will be done in preclinical sarcoma models.
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U2 - 10.1021/acs.jmedchem.5b00126
DO - 10.1021/acs.jmedchem.5b00126
M3 - Article
C2 - 25905694
AN - SCOPUS:84929378676
VL - 58
SP - 4073
EP - 4079
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
SN - 0022-2623
IS - 9
ER -