TY - JOUR
T1 - Insight on [1,3]thiazolo[4,5-e]isoindoles as tubulin polymerization inhibitors
AU - Barraja, Paola
AU - Carbone, Anna
AU - Montalbano, Alessandra
AU - Raimondi, Maria Valeria
AU - Palumbo Piccionello, Antonio
AU - Barreca, Marilia
AU - Spano', Virginia
AU - Hamel, Ernest
AU - Bortolozzi, Roberta
AU - Rocca, Roberta
AU - Alcaro, Stefano
AU - Viola, Giampietro
AU - Bai, Ruoli
PY - 2021
Y1 - 2021
N2 - A series of [1,3]thiazolo[4,5-e]isoindoles has been synthesized through a versatile and high yielding multistep sequence. Evaluation of the antiproliferative activity of the new compounds on the full NCI human tumor cell line panel highlighted several compounds that are able to inhibit tumor cell proliferation at micromolar-submicromolar concentrations. The most active derivative 11g was found to cause cell cycle arrest at the G2/M phase and induce apoptosis in HeLa cells, following the mitochondrial pathway, making it a lead compound for the discovery of new antimitotic drugs.
AB - A series of [1,3]thiazolo[4,5-e]isoindoles has been synthesized through a versatile and high yielding multistep sequence. Evaluation of the antiproliferative activity of the new compounds on the full NCI human tumor cell line panel highlighted several compounds that are able to inhibit tumor cell proliferation at micromolar-submicromolar concentrations. The most active derivative 11g was found to cause cell cycle arrest at the G2/M phase and induce apoptosis in HeLa cells, following the mitochondrial pathway, making it a lead compound for the discovery of new antimitotic drugs.
UR - http://hdl.handle.net/10447/460328
M3 - Article
SN - 0223-5234
VL - 212
SP - 1
EP - 17
JO - European Journal of Medicinal Chemistry
JF - European Journal of Medicinal Chemistry
ER -