RT Journal Article
T1 Synthetic cannabinoid quinones: Preparation, in vitro antiproliferative effects and in vivo prostate antitumor activity
A1 Morales, Paula
A1 Vara, Diana
A1 Gómez Cañas, María
A1 Zúñiga, María
A1 Olea-Azar, Claudio
A1 Goya, Pilar
A1 Fernández Ruiz, José Javier
A1 Díaz-Laviada Marturet, Inés
A1 Jagerovic, Nadine
AB Chromenopyrazolediones have been designed and synthesized as anticancer agents using the multi biological target concept that involves quinone cytotoxicity and cannabinoid antitumor properties. In cell cytotoxicity assays, these chromenopyrazolediones have antiproliferative activity against human prostate cancer and hepatocellular carcinoma. It has been shown that the most potent, derivative 4 (PM49), inhibits prostate LNCaP cell viability (IC50 ¼ 15 mM) through a mechanism involving oxidative stress, PPARg receptor and partially CB1 receptor. It acts on prostate cell growth by causing G0/G1 phase arrest and triggering apoptosis as assessed by flow cytometry measurements. In the in vivo treatment, compound 4 at 2 mg/kg, blocks the growth of LNCaP tumors and reduces the growth of PC-3 tumors generated in mice. These studies suggest that 4 is a good potential anticancer agent against hormone sensitive prostate cancer.
PB Elsevier
SN 0223-5234
YR 2013
FD 2013
LK https://hdl.handle.net/20.500.14352/93639
UL https://hdl.handle.net/20.500.14352/93639
LA eng
NO Morales P, Vara D, Goméz-Cañas M, Zúñiga MC, Olea-Azar C, Goya P, Fernández-Ruiz J, Díaz- Laviada I, Jagerovic N. Synthetic cannabinoid quinones: preparation, in vitro antiproliferative effects and in vivo prostate antitumor activity. Eur J MedChem. 2013, 70:111-9.
DS Docta Complutense
RD 8 abr 2025