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Chemical Compound Review

CHEMBL20682     6-oxo-6-[2-oxo-2-[(2R,4S)- 2,5,12...

Synonyms: AD-143, NSC-336379, AC1L7DR2
 
 
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Disease relevance of AD-143

 

High impact information on AD-143

  • After preincubation with AD 143 at concentrations as low as 5.2 microM (ML-1) or 13 microM (P3HR-1), the ability of the cells to take up extracellular labeled nucleosides was decreased by more than 50% [1].
  • These observations suggest that the decreased incorporation of [3H]thymidine and [3H]uridine into acid-precipitable material that we observed earlier in the AD 143-treated cells may in part be the result of the AD 143-induced alteration of cell membrane activities, which in turn causes an inhibition of nucleoside uptake [1].
  • An increase in the membrane fluidity was observed after treatment of the cells with AD 143, as revealed by electron paramagnetic resonance spectroscopy studies [1].
  • N-Trifluoroacetyladriamycin-14-O- Hemiadipate (AD 143), a new derivative of adriamycin with greater antitumor activity and lower cardiotoxicity, was shown not to interact with DNA and yet inhibit the activities of both RNA polymerases I and II of chicken myeloblastosis cells in vitro with ID50 values equal to 6.5 microM and 7 microM, respectively [2].

References

  1. Nucleoside uptake and membrane fluidity studies on N-trifluoroacetyladriamycin-14-O-hemiadipate-treated human leukemia and lymphoma cells. Lameh, J., Chuang, R.Y., Israel, M., Chuang, L.F. Cancer Res. (1989) [Pubmed]
  2. Selective inhibition of eukaryotic RNA polymerase: a possible new mechanism of antitumor drug action. Chuang, L.F., Nooteboom, G.N., Israel, M., Chuang, R.Y. Biochem. Biophys. Res. Commun. (1984) [Pubmed]
 
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