Selective, Nontoxic
CB<sub>2</sub> Cannabinoid <i>o</i>‑Quinone with
in Vivo Activity against Triple-Negative
Breast Cancer
Paula Morales
Sandra Blasco-Benito
Clara Andradas
María Gómez-Cañas
Juana María Flores
Pilar Goya
Javier Fernández-Ruiz
Cristina Sánchez
Nadine Jagerovic
10.1021/acs.jmedchem.5b00078.s001
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
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 (<b>10</b>) has been selected from a series of chromenopyrazolediones with
full selectivity for the nonpsychotropic CB<sub>2</sub> 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 <b>10</b> exerts antitumor effect by inducing cell
apoptosis through activation of CB<sub>2</sub> 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.
2015-03-12 00:00:00
CB 2 receptors
compound
nonpsychotropic CB 2 cannabinoid receptor
breast cancer
TNBC cell lines
antitumor
Nontoxic CB 2 Cannabinoid
quinone
vivo