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-intercalating compound, are described. The compound showed dose-dependent antiproliferative activity against all of the tested murine and human tumor cell lines, as evaluated by using the tetrazolium-based colorimetric assay. In addition, a comparative evaluation of the cytotoxic property was performed also against primary cultures of normal bone marrow cells. The results demonstrated that APPT possesses preferential antitumor activity and is endowed with an in vitro therapeutic index very similar to those of well known DNA-binding anti-neoplastic compounds, such as daunorubicin (DNR) and amsacrine (mAMSA). Therefore, APPT can be considered to be a potential selective cytoreductive drug.
Nocentini
G
G
Department of Clinical Medicine, Pathology and Pharmacology, University of Perugia, Italy.
Castagnino
E
E
Salvatori
A
A
Corsano
S
S
Fioretti
M C
MC
D000166:Acridines / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007939:Leukemia L1210 / Q000188:drug therapy; D007941:Leukemia P388 / Q000188:drug therapy; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D013778:Tetrazolium Salts; D013844:Thiazoles; D014407:Tumor Cells, Cultured
D000166:Acridines; D000970:Antineoplastic Agents; C098447:N-acridylpentanoyloxypyridine-2-thione; D013778:Tetrazolium Salts; D013844:Thiazoles; C022616:thiazolyl blue