Triarylethylene-indolin-2,3-dione molecular conjugates: design, synthesis, docking studies and anti-proliferation evaluation

A series of 1 H -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 combina...

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Published inRSC advances Vol. 9; no. 72; pp. 4249 - 42414
Main Authors Kumar, Sumit, Palma, Gabriella, Perumal, Shanen, Kaur, Mandeep, Singh-Pillay, Ashona, Raj, Raghu, Singh, Parvesh, Kumar, Vipan
Format Journal Article
LanguageEnglish
Published England Royal Society of Chemistry 20.12.2019
The Royal Society of Chemistry
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Summary:A series of 1 H -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 IC 50 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 β. A series of 1 H -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.
Bibliography:13b
14c
15d
10.1039/c9ra08776a
C NMR data of all the synthesized conjugates along with scanned
C, DEPT, D
13
14e
Electronic supplementary information (ESI) available
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H
O) NMR spectra for representative compounds
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See DOI
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2
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14a
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15c
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ISSN:2046-2069
2046-2069
DOI:10.1039/c9ra08776a