Abstract
This review summarizes our experiments investigating structure–activity relationships of 3-benzazepines. Three 7,8-dihydroxy-3-benzazepines [ 7– 9] were cytotoxic to human promyelotic leukaemia HL-60 cells. Compound [ 9] showed the highest cytotoxicity and the activity was twice as high as that of dopamine (DA, [ 11]). Three active compounds [ 7– 9] produced radicals, whereas other less potent benzazepines [ 1– 6, 10] did not produce radicals. Furthermore, cytotoxic 3-benzazepines [ 7– 9] also enhanced the decay of ascorbic acid in rat brain homogenate. Two 7,8-dimethoxy-3-benzazepines [ 5, 10] were able to form a complex with the replicative form of plasmid DNA. The multidrug resistance (MDR) P-glycoprotein ( Pgp) efflux pump of mouse lymphoma cells was inhibited by three compounds [ 5, 8, 10]. Compound [ 8] has the highest activity in MDR reversal and is two times more potent than verapamil. Three cytotoxic 3-benzazepines [ 7– 9] showed inhibitory effects against reverse transcriptase (RT) of Moloney leukemia.
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