Triarylethylene-indolin-2,3-dione molecular conjugates: design, synthesis, docking studies and anti-proliferation evaluation.
RSC Adv
; 9(72): 42409-42414, 2019 Dec 18.
Article
em En
| MEDLINE
| ID: mdl-35542879
A series of 1H-1,2,3-triazole-linked ospemifene-isatin and O-methylated ospemifene-isatin conjugates were synthesized and assayed for their anti-proliferative activities against estrogen-responsive as well as estrogen-non-responsive cells. The non-cytotoxic conjugate 14e, with an optimal combination of bromo substituents at the C-5/C-7 positions of isatin, proved to be a promising hit with an IC50 value of 31.62 µM against MCF-7 and 19.23 µM against MDA-MB-231. The observed anti-proliferative activities of active conjugates were further corroborated via docking studies carried out on estrogen receptor subtypes α and ß.
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01-internacional
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MEDLINE
Idioma:
En
Revista:
RSC Adv
Ano de publicação:
2019
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Article