A new class of potential antitumor agents, provided with thieno(2', 3': 5,6)pyrido(2,3-d) pyridazin-9(4H)-one nucleus as chromophore, was synthesized. Thus, the suitable amines were reacted, in different conditions, with 5,8-dichlorothieno((2', 3': 5,6)pyrido(2,3-d) pyridazin-9(4H)-one (5) to afford the 8-alkylamino derivatives 6a-f, the 5-alkylamino derivatives 7a-f, and the 5,8-bis-alkylamino derivatives 8a,b. Selected compounds were evaluated for cytotoxic potency in vitro against the uman colon adenocarcinoma HT 29 cell line and studied in DNA binding assays. The cytotoxic potency versus HT29 was also correlated with binding affinity for calf tymus DNA.
Synthesis and biological evaluation of mono- and bis-[(alkylamino)alkylamino] substituted thienopyridopyridazines, a new class of potential antitumor agents
PALMIERI, Giovanni Filippo;
1996-01-01
Abstract
A new class of potential antitumor agents, provided with thieno(2', 3': 5,6)pyrido(2,3-d) pyridazin-9(4H)-one nucleus as chromophore, was synthesized. Thus, the suitable amines were reacted, in different conditions, with 5,8-dichlorothieno((2', 3': 5,6)pyrido(2,3-d) pyridazin-9(4H)-one (5) to afford the 8-alkylamino derivatives 6a-f, the 5-alkylamino derivatives 7a-f, and the 5,8-bis-alkylamino derivatives 8a,b. Selected compounds were evaluated for cytotoxic potency in vitro against the uman colon adenocarcinoma HT 29 cell line and studied in DNA binding assays. The cytotoxic potency versus HT29 was also correlated with binding affinity for calf tymus DNA.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.