Paper
Biological activity of hydantoin derivatives on P-glycoprotein (ABCB1) of mouse lymphoma cells.
Published Dec 1, 2010 · G. Spengler, Miguel Evaristo, J. Handzlik
Anticancer research
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Abstract
BACKGROUND Hydantoin derivatives possess a variety of biochemical and pharmacological properties. Although hydantoin compounds are studied extensively, there are not many studies that investigate their anticancer properties. MATERIALS AND METHODS Thirty hydantoin compounds were evaluated for their efflux modulating effects in cancer cells using a rhodamine 123 accumulation assay and real-time fluorometry based on the intracellular accumulation of ethidium bromide. RESULTS The 30 derivatives were screened by real-time fluorometry for rhodamine 123 accumulation. Among the selected derivatives, compounds SZ-7, LL-9, BS-1, MN-3, P3, RW-15b, AD-26, RW-13, AD-29 and KF-2 significantly increased the retention of rhodamine 123. Compounds AD-26, AD-29, RW-13, KF-2, BS-1, MN-3, RW-15b and JH-63 showed synergistic effect with doxorubicin on mouse lymphoma cells. Furthermore, compound SZ-7 had indifferent effect with doxorubicin. CONCLUSION These results indicated the role of chemical modifications within the hydantoin ring for its potential inhibition of the ABCB1 transporter. The most active structures contained aromatic substituents as well as some tertiary amine fragments.
In Vitro StudyHydantoin derivatives with aromatic substituents and tertiary amine fragments show potential anticancer properties by inhibiting the ABCB1 transporter in mouse lymphoma cells.
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