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.
Highlights
Cancer chemotherapy, as in the case of antimicrobial chemotherapy, has had trouble with resistance to treatment
As in the case of antimicrobial chemotherapy, has had trouble with resistance to treatment. This phenomenon occurs mainly through molecular mechanisms that may be affected by novel compounds that may be associated to cancer chemotherapy [1]
multi drug resistance (MDR) reverting calcium channels, we explored the possibility for this class of compounds to exhibit reverting such as the parent compound diltiazem [12], independent of the action on l-type calcium channels properties, as the parent
Summary
As in the case of antimicrobial chemotherapy, has had trouble with resistance to treatment. This phenomenon occurs mainly through molecular mechanisms that may be affected by novel compounds that may be associated to cancer chemotherapy [1]. Cancer treatment based on a combination of drugs with different mechanisms of action seems to be the best strategy to avoid multi drug resistance (MDR) [2,3]. This approach has proved to be successful for some kinds. The discovery that the high concentration (Pgp)Molecules that is2020, correlated of Pgp in resistant cells is independent of the chemical class of drugs used enlightens a further
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