%0 Journal Article
%A Morales, Paula
%A Blasco-Benito, Sandra
%A Andradas, Clara
%A Gómez-Cañas, María
%A Flores, Juana María
%A Goya, Pilar
%A Fernández-Ruiz, Javier
%A Sánchez, Cristina
%A Jagerovic, Nadine
%D 2015
%T Selective, Nontoxic
CB2 Cannabinoid o‑Quinone with
in Vivo Activity against Triple-Negative
Breast Cancer
%U https://acs.figshare.com/articles/journal_contribution/Selective_Nontoxic_CB_sub_2_sub_Cannabinoid_i_o_i_Quinone_with_in_Vivo_Activity_against_Triple_Negative_Breast_Cancer/2186719
%R 10.1021/acs.jmedchem.5b00078.s001
%2 https://ndownloader.figshare.com/files/3820885
%K CB 2 receptors
%K compound
%K nonpsychotropic CB 2 cannabinoid receptor
%K breast cancer
%K TNBC cell lines
%K antitumor
%K Nontoxic CB 2 Cannabinoid
%K quinone
%K vivo
%X Triple-negative breast
cancer (TNBC) represents a subtype of breast
cancer characterized by high aggressiveness. There is no current targeted
therapy for these patients whose prognosis, as a group, is very poor.
Here, we report the synthesis and evaluation of a potent antitumor
agent in vivo for this type of breast cancer designed as a combination
of quinone/cannabinoid pharmacophores. This new compound (10) has been selected from a series of chromenopyrazolediones with
full selectivity for the nonpsychotropic CB2 cannabinoid
receptor and with efficacy in inducing death of human TNBC cell lines.
The dual concept quinone/cannabinoid was supported by the fact that
compound 10 exerts antitumor effect by inducing cell
apoptosis through activation of CB2 receptors and through
oxidative stress. Notably, it did not show either cytotoxicity on
noncancerous human mammary epithelial cells nor toxic effects in vivo,
suggesting that it may be a new therapeutic tool for the management
of TNBC.
%I ACS Publications