TY - JOUR
T1 - 3-[4-(1H-indol-3-yl)-1,3-thiazol-2-yl]-1H-pyrrolo[2,3-b]pyridines, nortopsentin Analogues with antiproliferative activity
AU - Livrea, Maria Antonia
AU - Attanzio, Alessandro
AU - Parrino, Barbara
AU - Tesoriere, Luisa
AU - Montalbano, Alessandra
AU - Barraja, Paola
AU - Spano', Virginia
AU - Diana, Patrizia
AU - Ciancimino, Cristina
AU - Di Vita, Gloria
AU - Cirrincione, Girolamo
AU - Carbone, Anna
AU - Spanò, Virginia
AU - Parrino, Barbara
AU - Attanzio, Alessandro
AU - Ciancimino, Cristina
AU - Carbone, Anna
AU - Di Vita, Gloria
AU - Montalbano, Alessandra
AU - Barraja, Paola
AU - Cirrincione, Girolamo
AU - Diana, Patrizia
AU - Tesoriere, Luisa
AU - Livrea, Maria Antonia
PY - 2015
Y1 - 2015
N2 - A new series of nortopsentin analogues, in which the imidazole ring of the natural product was replaced by thiazole and the indole unit bound to position 2 of the thiazole ring was substituted by a 7-azaindole moiety, was efficiently synthesized. Two of the new nortopsentin analogues showed good antiproliferative effect against the totality of the NCI full panel of human tumor cell lines (∼60) having GI50 values ranging from low micromolar to nanomolar level. The mechanism of the antiproliferative effect of these derivatives, investigated on human hepatoma HepG2 cells, was pro-apoptotic, being associated with externalization of plasma membrane phosphatidylserine and mitochondrial dysfunction. Moreover, the compounds induced a concentration-dependent accumulation of cells in the subG0/G1phase, while confined viable cells in G2/M phase.
AB - A new series of nortopsentin analogues, in which the imidazole ring of the natural product was replaced by thiazole and the indole unit bound to position 2 of the thiazole ring was substituted by a 7-azaindole moiety, was efficiently synthesized. Two of the new nortopsentin analogues showed good antiproliferative effect against the totality of the NCI full panel of human tumor cell lines (∼60) having GI50 values ranging from low micromolar to nanomolar level. The mechanism of the antiproliferative effect of these derivatives, investigated on human hepatoma HepG2 cells, was pro-apoptotic, being associated with externalization of plasma membrane phosphatidylserine and mitochondrial dysfunction. Moreover, the compounds induced a concentration-dependent accumulation of cells in the subG0/G1phase, while confined viable cells in G2/M phase.
UR - http://hdl.handle.net/10447/145699
M3 - Article
VL - 13
SP - 1901
EP - 1924
JO - Marine Drugs
JF - Marine Drugs
SN - 1660-3397
ER -