Synthesis of Tamoxifen-Artemisinin and Estrogen-Artemisinin Hybrids Highly Potent Against Breast and Prostate Cancer.
ChemMedChem
; 15(15): 1473-1479, 2020 08 05.
Article
en En
| MEDLINE
| ID: mdl-32374071
ABSTRACT
In the search for new and effective treatments of breast and prostate cancer, a series of hybrid compounds based on tamoxifen, estrogens, and artemisinin were successfully synthesized and analyzed for their inâ
vitro activities against human prostate (PC-3) and breast cancer (MCF-7) cell lines. Most of the hybrid compounds exhibit a strong anticancer activity against both cancer cell lines - for example, EC50 (PC-3) down to 1.07â
µM, and EC50 (MCF-7) down to 2.08â
µM - thus showing higher activities than their parent compounds 4-hydroxytamoxifen (afimoxifene, 7; EC50 =75.1 (PC-3) and 19.3â
µM (MCF-7)), dihydroartemisinin (2; EC50 =263.6 (PC-3) and 49.3â
µM (MCF-7)), and artesunic acid (3; EC50 =195.1 (PC-3) and 32.0â
µM (MCF-7)). The most potent compounds were the estrogen-artemisinin hybrids 27 and 28 (EC50 =1.18 and 1.07â
µM, respectively) against prostate cancer, and hybrid 23 (EC50 =2.08â
µM) against breast cancer. These findings demonstrate the high potential of hybridization of artemisinin and estrogens to further improve their anticancer activities and to produce synergistic effects between linked pharmacophores.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Banco de datos:
MEDLINE
Asunto principal:
Neoplasias de la Próstata
/
Tamoxifeno
/
Neoplasias de la Mama
/
Artemisininas
/
Estrógenos
/
Antineoplásicos
Límite:
Female
/
Humans
/
Male
Idioma:
En
Revista:
ChemMedChem
Asunto de la revista:
FARMACOLOGIA
/
QUIMICA
Año:
2020
Tipo del documento:
Article
País de afiliación:
Alemania