IN-VITRO EVALUATION OF THE POTENTIAL ANTITUMOR-ACTIVITY OF AN N-ACRIDYL-PENTANOYLOXYPYRIDINE-2-THIONE DERIVATIVE

The synthesis and in vitro evaluation of the antitumor activity of an N-acridyl-pentanoyloxypridine-2-thione derivative (APPT), hypothesized to act as a DNA-in-tercalcating compound, are described. The compound showed dose-dependent antiproliferative activity against all of the t ested murine and human tumor cell lines, as evaluated by using the tet razolium-based colorimetric assay. In addition, a comparative evaluati on of the cytotoxic property was performed also against primary cultur es of normal bone marrow cells. The results demonstrated that APPT pos sesses preferential antitumor activity and is endowed with an in vitro therapeutic index very similar to those of well known DNA-binding ant ineoplastic compounds, such as daunorubicin (DNR) and amsacrine (mAMSA ). Therefore, APPT can be considered to be a potential selective cytor eductive drug.