@misc{10481/70199,
year = {2021},
month = {7},
url = {http://hdl.handle.net/10481/70199},
abstract = {A series of 11 new substituted 1,5-dihydro-4,1-benzoxazepine derivatives was synthesised to study the
influence of the methyl group in the 1-(benzenesulphonyl) moiety, the replacement of the purine by the
benzotriazole bioisosteric analogue, and the introduction of a bulky substituent at position 6 of the purine,
on the biological effects. Their inhibition against isolated HER2 was studied and the structure–activity
relationships have been confirmed by molecular modelling studies. The most potent compound against
isolated HER2 is 9a with an IC50 of 7.31 mM. We have investigated the effects of the target compounds on
cell proliferation. The most active compound (7c) against all the tumour cell lines studied (IC50
0.42–0.86 mM) does not produce any modification in the expression of pro-caspase 3, but increases the
caspase 1 expression, and promotes pyroptosis.},
organization = {Junta de Andalucia	P18-RT-1679},
organization = {Oficina de Transferencia de Resultados de Investigacion of the University of Granada	PR/17/006},
organization = {Instituto de Salud Carlos III
European Commission	RTI2018-101309-B-C22},
organization = {Instituto de Salud Carlos III	FMM-AP16683-2017},
organization = {Junta de Andalucia	PI-0089-2017},
publisher = {Taylor & Francis},
keywords = {Antitumour},
keywords = {Pyroptosis},
keywords = {HER2 receptor},
keywords = {Molecular modelling},
keywords = {Benzoxazepines},
title = {Design, synthesis, HER2 inhibition and anticancer evaluation of new substituted 1,5-dihydro-4,1- benzoxazepines},
doi = {10.1080/14756366.2021.1948841},
author = {Cruz López, Olga María and Ner, Matilde and Jiménez Martínez, Yaiza and Marchal Corrales, Juan Antonio and Boulaiz Tassi, Houria and Campos Rosa, Joaquín María and Conejo García, Ana},
}