438201-58-2Relevant academic research and scientific papers
Effect of modification of 6-[(aminoalkyl)amino]-7H-benzo[e]-perimidin-7-ones on their cytotoxic activity toward sensitive and multidrug resistant tumor cell lines. Synthesis and biological evaluation
Dzieduszycka, Maria,Martelli, Sante,Arciemiuk, Ma,Bontemps-Gracz, Maria M.,Kupiec, Agnieszka,Borowski, Edward
, p. 1025 - 1035 (2002)
Benzoperimidines, a novel group of antitumor anthracenedione analogues, are of interest due to their ability to overcome multidrug resistance of tumor cells (Stefanska, B., Dzieduszyc a, M., Bontemps-Gracz, M. M., Borows i, E., Martelli, S., Supino, R., Pratesi, G., De Cesare, MA., Zunino, F., Kusnierczy , H., Radziowski, Cz. J. Med. Chem. 1999, 42, 3494). Although the structural factor essential for exhibiting this desirable property is the presence in the molecule of a fused heterocyclic ring, the cytotoxicity against resistant cells is highly influenced by the nature and location of the substituents. A series of novel synthetic derivatives, comprising monohydroxylated benzoperimidines and 2-aminobenzoperimidines, allowed the establishment of an invitro structure-activity relationship for a panel of leuemia sensitive, as well as P-gp dependent multidrug resistance (MDR) and multidrug resistance associated protein dependent resistance (MRP) resistant cell lines. The membrane affinity for the compounds has also been determined. Copyright
