3,4-Dihydroxybenzylamine hydrobromide (NSC 263475 hydrobromide) is an improved dopamine analog cytotoxic and inhibits DNA polymerase activity in melanoma cells. 3,4-Dihydroxybenzylamine hydrobromide (NSC 263475 hydrobromide) displays growth inhibitory activity in melanoma cell lines with varying degrees oftyrosinase activity.
3,4-Dihydroxybenzylamine hydrobromide (NSC 263475 hydrobromide) is an improved dopamine analog cytotoxic and inhibits DNA polymerase activity in melanoma cells. Inhibition of DNA polymerase by activated 3,4-DHBA was shown by dialysis and kinetic studies to involve an irreversible reaction which occurs at two inhibitor interaction sites as determined by a Hill plot analysis. Double-stranded DNA protected the enzyme from inhibition by 3,4-DHBA, suggesting that the inhibitory sites are at or near the template-initiator binding site[4]. 3,4-Dihydroxybenzylamine hydrobromide (NSC 263475 hydrobromide) displays growth inhibitory activity in melanoma cell lines with varying degrees of tyrosinase activity[5].3,4-Dihydroxybenzylamine (DHBA), a dopamine analog, was much less toxic than dopamine when tested against the B16 melanoma in vivo and in vitro. Daily doses of 1,000 mg DHBA/kg were better tolerated than doses of 400 mg dopamine/kg. When tested against the B16 melanoma in (C57BL/6 x DBA/2)F1 mice, DHBA had a significantly improved therapeutic effect as shown by a life-span increased 70% as compared to 48% with dopamine. DHBA shared the catecholamine property of selectively inhibiting thymidine incorporation as compared to leucine or uridine incorporation[6].
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