3-Aryl-4-nitrobenzothiochromans S,S-dioxide: From Calcium-Channel Modulators Properties to Multidrug-Resistance Reverting Activity

Matteo Micucci, Maurizio Viale, Alberto Chiarini, Domenico Spinelli, Maria Frosini, Cinzia Tavani, Massimo Maccagno, Lara Bianchi, Rosaria Gangemi, Roberta Budriesi

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Abstract

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.

Original languageEnglish
JournalMolecules (Basel, Switzerland)
Volume25
Issue number5
DOIs
Publication statusPublished - Feb 27 2020

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Keywords

  • 3-aryl-4-nitrothiochromans S,S-dioxide
  • anticancer therapy
  • cardiovascular activity
  • in vitro experiments
  • l-Type Calcium Channels (LTCC)
  • multidrug resistance (MDR1)

ASJC Scopus subject areas

  • Analytical Chemistry
  • Chemistry (miscellaneous)
  • Molecular Medicine
  • Pharmaceutical Science
  • Drug Discovery
  • Physical and Theoretical Chemistry
  • Organic Chemistry

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