TY - JOUR
T1 - [1,2]Oxazolo[5,4-e]isoindoles as promising tubulin polymerization inhibitors
AU - Cirrincione, Girolamo
AU - Carbone, Anna
AU - Parrino, Barbara
AU - Diana, Patrizia
AU - Montalbano, Alessandra
AU - Spano', Virginia
AU - Barraja, Paola
AU - Lopergolo, Alessia
AU - Cominetti, Denis
AU - Pennati, Marzia
AU - Zuco, Valentina
AU - Zaffaroni, Nadia
PY - 2016
Y1 - 2016
N2 - A series of [1,2]Oxazolo [5,4-e]isoindoles has been synthesized through a versatile and high yielding sequence. All the new structures showed in the 1HNMR spectra, the typical signal in the 8.34–8.47 ppm attributable to the H-3 of the [1,2]oxazole moiety. Among all derivatives, methoxy benzyl substituents at positions 3 and 4 or/and 5 were very effective in reducing the growth of different tumor cell lines, including diffuse malignant peritoneal mesothelioma (DMPM), an uncommon and rapidly malignancy poorly responsive to available therapeutic options. The most active compound 6j was found to impair tubulin polymerization, cause cell cycle arrest at G2/M phase and induce apoptosis in DMPM cells, making it as a new lead for the discovery of new potent antimitotic drugs.
AB - A series of [1,2]Oxazolo [5,4-e]isoindoles has been synthesized through a versatile and high yielding sequence. All the new structures showed in the 1HNMR spectra, the typical signal in the 8.34–8.47 ppm attributable to the H-3 of the [1,2]oxazole moiety. Among all derivatives, methoxy benzyl substituents at positions 3 and 4 or/and 5 were very effective in reducing the growth of different tumor cell lines, including diffuse malignant peritoneal mesothelioma (DMPM), an uncommon and rapidly malignancy poorly responsive to available therapeutic options. The most active compound 6j was found to impair tubulin polymerization, cause cell cycle arrest at G2/M phase and induce apoptosis in DMPM cells, making it as a new lead for the discovery of new potent antimitotic drugs.
UR - http://hdl.handle.net/10447/212856
UR - http://www.journals.elsevier.com/european-journal-of-medicinal-chemistry/
M3 - Article
VL - 124
SP - 840
EP - 851
JO - European Journal of Medicinal Chemistry
JF - European Journal of Medicinal Chemistry
SN - 0223-5234
ER -