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

摘要

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-2 -thiopyran -dioxide , and have observed no activity. Then we have extended our investigation to the 3-aryl-4-nitrobenzothiochromans -dioxide and , 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 exerted the most effect on negative inotropic activity, while and could be interesting molecules for the development of more active ABCB1 inhibitors. Both and represent structures of large possible biological interest, providing a scaffold for the identification of new ABCB1 inhibitors.