A platinum(II) complex with the antiviral drug acyclovir was synthesized and its
antiviral and anticancer properties were investigated in comparison to those of acyclovir and
cisplatin. The platinum-acyclovir complex maintained the antiviral activity of the parent
drug acyclovir, though showing a minor efficacy on a molar basis (ID50 = 7.85 and 1.02 μΜ
for platinum-acyclovir and cisplatin, respectively). As anticancer agent, the platinum-acyclovir
complex was markedly less potent than cisplatin on a mole-equivalent basis, but it
was as effective as cisplatin when equitoxic dosages were administered in vivo to P388
leukaemia-bearing mice (%T/C = 209 and 211 for platinum-acyclovir and cisplatin,
respectively). The platinum-acyclovir complex was also active against a cisplatin-resistant
subline of the P388 leukaemia (%T/C = 140), thus suggesting a different mechanism of
action. The DNA interaction properties (sequence specificity and interstrand cross-linking
ability) of platinum-acyclovir were also investigated in comparison to those of cisplatin and
[Pt(dien)Cl]+, an antitumour-inactive platinum-triamine compound. The results of this study
point to a potential new drug endowed, at the same time, with antiviral and anticancer
activity and characterized by DNA interaction properties different from those of cisplatin.
Copyright
Copyright © 1995 Hindawi Publishing Corporation. This is an open access article distributed under the
Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
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