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3-Aryl-4-nitrobenzothiochromans S,S-dioxide: From Calcium-Channel Modulators Properties to Multidrug-Resistance Reverting Activity
Our research groups have been involved for many years in studies aimed at identifying new active organic compounds endowed with pharmacological properties. In this work, we focused our attention on the evaluation of cardiovascular and molecular drug resistance (MDR) reverting activities of some nitr...
Autores principales: | , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2020
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7179187/ https://www.ncbi.nlm.nih.gov/pubmed/32120861 http://dx.doi.org/10.3390/molecules25051056 |
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author | Micucci, Matteo Viale, Maurizio Chiarini, Alberto Spinelli, Domenico Frosini, Maria Tavani, Cinzia Maccagno, Massimo Bianchi, Lara Gangemi, Rosaria Budriesi, Roberta |
author_facet | Micucci, Matteo Viale, Maurizio Chiarini, Alberto Spinelli, Domenico Frosini, Maria Tavani, Cinzia Maccagno, Massimo Bianchi, Lara Gangemi, Rosaria Budriesi, Roberta |
author_sort | Micucci, Matteo |
collection | PubMed |
description | Our research groups have been involved for many years in studies aimed at identifying new active organic compounds endowed with pharmacological properties. In this work, we focused our attention on the evaluation of cardiovascular and molecular drug resistance (MDR) reverting activities of some nitrosubstituted sulphur-containing heterocycles. Firstly, we have examined the effects of 4-nitro-3-(4-methylphenyl)-3,6-dihydro-2H-thiopyran S,S-dioxide 5, and have observed no activity. Then we have extended our investigation to the 3-aryl-4-nitrobenzothiochromans S,S-dioxide 6 and 7, and have observed an interesting biological profile. Cardiovascular activities were assessed for all compounds using ex vivo studies, while the MDR reverting effect was evaluated only for selected compounds using tumor cell lines. All compounds were shown to affect cardiovascular parameters. Compound 7i exerted the most effect on negative inotropic activity, while 6d and 6f could be interesting molecules for the development of more active ABCB1 inhibitors. Both 6 and 7 represent structures of large possible biological interest, providing a scaffold for the identification of new ABCB1 inhibitors. |
format | Online Article Text |
id | pubmed-7179187 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2020 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-71791872020-04-28 3-Aryl-4-nitrobenzothiochromans S,S-dioxide: From Calcium-Channel Modulators Properties to Multidrug-Resistance Reverting Activity Micucci, Matteo Viale, Maurizio Chiarini, Alberto Spinelli, Domenico Frosini, Maria Tavani, Cinzia Maccagno, Massimo Bianchi, Lara Gangemi, Rosaria Budriesi, Roberta Molecules Article Our research groups have been involved for many years in studies aimed at identifying new active organic compounds endowed with pharmacological properties. In this work, we focused our attention on the evaluation of cardiovascular and molecular drug resistance (MDR) reverting activities of some nitrosubstituted sulphur-containing heterocycles. Firstly, we have examined the effects of 4-nitro-3-(4-methylphenyl)-3,6-dihydro-2H-thiopyran S,S-dioxide 5, and have observed no activity. Then we have extended our investigation to the 3-aryl-4-nitrobenzothiochromans S,S-dioxide 6 and 7, and have observed an interesting biological profile. Cardiovascular activities were assessed for all compounds using ex vivo studies, while the MDR reverting effect was evaluated only for selected compounds using tumor cell lines. All compounds were shown to affect cardiovascular parameters. Compound 7i exerted the most effect on negative inotropic activity, while 6d and 6f could be interesting molecules for the development of more active ABCB1 inhibitors. Both 6 and 7 represent structures of large possible biological interest, providing a scaffold for the identification of new ABCB1 inhibitors. MDPI 2020-02-27 /pmc/articles/PMC7179187/ /pubmed/32120861 http://dx.doi.org/10.3390/molecules25051056 Text en © 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Micucci, Matteo Viale, Maurizio Chiarini, Alberto Spinelli, Domenico Frosini, Maria Tavani, Cinzia Maccagno, Massimo Bianchi, Lara Gangemi, Rosaria Budriesi, Roberta 3-Aryl-4-nitrobenzothiochromans S,S-dioxide: From Calcium-Channel Modulators Properties to Multidrug-Resistance Reverting Activity |
title | 3-Aryl-4-nitrobenzothiochromans S,S-dioxide: From Calcium-Channel Modulators Properties to Multidrug-Resistance Reverting Activity |
title_full | 3-Aryl-4-nitrobenzothiochromans S,S-dioxide: From Calcium-Channel Modulators Properties to Multidrug-Resistance Reverting Activity |
title_fullStr | 3-Aryl-4-nitrobenzothiochromans S,S-dioxide: From Calcium-Channel Modulators Properties to Multidrug-Resistance Reverting Activity |
title_full_unstemmed | 3-Aryl-4-nitrobenzothiochromans S,S-dioxide: From Calcium-Channel Modulators Properties to Multidrug-Resistance Reverting Activity |
title_short | 3-Aryl-4-nitrobenzothiochromans S,S-dioxide: From Calcium-Channel Modulators Properties to Multidrug-Resistance Reverting Activity |
title_sort | 3-aryl-4-nitrobenzothiochromans s,s-dioxide: from calcium-channel modulators properties to multidrug-resistance reverting activity |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7179187/ https://www.ncbi.nlm.nih.gov/pubmed/32120861 http://dx.doi.org/10.3390/molecules25051056 |
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