Cargando…

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...

Descripción completa

Detalles Bibliográficos
Autores principales: Micucci, Matteo, Viale, Maurizio, Chiarini, Alberto, Spinelli, Domenico, Frosini, Maria, Tavani, Cinzia, Maccagno, Massimo, Bianchi, Lara, Gangemi, Rosaria, Budriesi, Roberta
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
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
_version_ 1783525616656580608
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
work_keys_str_mv AT micuccimatteo 3aryl4nitrobenzothiochromansssdioxidefromcalciumchannelmodulatorspropertiestomultidrugresistancerevertingactivity
AT vialemaurizio 3aryl4nitrobenzothiochromansssdioxidefromcalciumchannelmodulatorspropertiestomultidrugresistancerevertingactivity
AT chiarinialberto 3aryl4nitrobenzothiochromansssdioxidefromcalciumchannelmodulatorspropertiestomultidrugresistancerevertingactivity
AT spinellidomenico 3aryl4nitrobenzothiochromansssdioxidefromcalciumchannelmodulatorspropertiestomultidrugresistancerevertingactivity
AT frosinimaria 3aryl4nitrobenzothiochromansssdioxidefromcalciumchannelmodulatorspropertiestomultidrugresistancerevertingactivity
AT tavanicinzia 3aryl4nitrobenzothiochromansssdioxidefromcalciumchannelmodulatorspropertiestomultidrugresistancerevertingactivity
AT maccagnomassimo 3aryl4nitrobenzothiochromansssdioxidefromcalciumchannelmodulatorspropertiestomultidrugresistancerevertingactivity
AT bianchilara 3aryl4nitrobenzothiochromansssdioxidefromcalciumchannelmodulatorspropertiestomultidrugresistancerevertingactivity
AT gangemirosaria 3aryl4nitrobenzothiochromansssdioxidefromcalciumchannelmodulatorspropertiestomultidrugresistancerevertingactivity
AT budriesiroberta 3aryl4nitrobenzothiochromansssdioxidefromcalciumchannelmodulatorspropertiestomultidrugresistancerevertingactivity