Skip to main content
SpringerLink
Log in

Naphtho[2,3-f]indole-5,10-dione aminoalkyl derivatives: A new class of topoisomerase I inhibitors

  • Pharmacology and Toxicology
  • Published:
Bulletin of Experimental Biology and Medicine Aims and scope

Abstract

Naphtho[2,3-f]indole-5,10-dione aminoalkyl derivatives in cytotoxic concentrations inhibit topoisomerase I, which is an important factor of antitumor activity of compounds of this chemical class. The degree of topoisomerase I inhibition with naphtho[2,3-f]indole-5,10-dione derivatives depends on the structure and position of active (aminoalkyl) groups. The mechanism of topoisomerase I inhibition with aminoalkylnaphtho[2,3-f]indole-5,10-diones differs from specific blocking of the catalytic activity of the enzyme and depends on interactions of these compounds with DNA.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Log in via an institution

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Institutional subscriptions

References

  1. A. A. Adjei, M. Charron, and E. K. Rowinsky, Clin. Cancer Res., 4, No. 3, 683–691 (1998).

    PubMed  CAS  Google Scholar 

  2. W. A. Denny, Expert Opin. Emerg. Drugs, 9, No. 1, 105–133 (2004).

    PubMed  CAS  Google Scholar 

  3. M. Facompre, C. Carrasco, P. Colson, et al., Mol. Pharmacol., 62, No. 5, 1215–1227 (2002).

    Article  PubMed  CAS  Google Scholar 

  4. P. D. Foglesong, C. Reckord, and S. Swink, Cancer Chemother. Pharmacol., 30, No. 2, 123–125 (1992).

    Article  PubMed  CAS  Google Scholar 

  5. L. F. Liu, Annu. Rev. Biochem., No. 58, 351–375 (1989).

  6. A. E. Shchekotikhin, L. G. Dezhenkova, O. Y. Susova, et al., Bioorg. Med. Chem., 15, No. 7, 2651–2659 (2007).

    Article  PubMed  CAS  Google Scholar 

  7. A. E. Shchekotikhin, V. A. Glazunova, Y. N. Luzikov, et al., Ibid., 14, No. 15, 5241–5251 (2006).

    Article  PubMed  CAS  Google Scholar 

  8. A. E. Shchekotikhin, A. A. Shtil, Y. N. Luzikov, et al., Ibid., 13, No. 6, 2285–2291 (2005).

    Article  PubMed  CAS  Google Scholar 

  9. L. Shen, Methods in Molecular Biology: DNA Topoisomerase Protocols, Part II: Enzymology and Drugs, Totova (2001), Vol. 95, P. 149.

    CAS  Google Scholar 

Download references

Author information

Authors and Affiliations

  1. G. F. Gauze Institute for Search for New Antibiotics, Russian Academy of Medical Sciences, Moscow, Russia

    L. G. Dezhenkova, A. E. Shchekotikhin & M. N. Preobrazhenskaya

  2. Institute of Carcinogenesis, N. N. Blokhin National Cancer Research Center, Russian Academy of Medical Sciences, Moscow, Russia

    O. Yu. Susova & A. A. Shtil

Authors
  1. L. G. Dezhenkova
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. O. Yu. Susova
    View author publications

    You can also search for this author in PubMed Google Scholar

  3. A. E. Shchekotikhin
    View author publications

    You can also search for this author in PubMed Google Scholar

  4. M. N. Preobrazhenskaya
    View author publications

    You can also search for this author in PubMed Google Scholar

  5. A. A. Shtil
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to A. A. Shtil.

Additional information

__________

Translated from Byulleten’ Eksperimental’noi Biologii i Meditsiny, Vol. 145, No. 3, pp. 304–308, March, 2008

Rights and permissions

Reprints and permissions

About this article

Cite this article

Dezhenkova, L.G., Susova, O.Y., Shchekotikhin, A.E. et al. Naphtho[2,3-f]indole-5,10-dione aminoalkyl derivatives: A new class of topoisomerase I inhibitors. Bull Exp Biol Med 145, 334–337 (2008). https://doi.org/10.1007/s10517-008-0084-8

Download citation

  • Received:

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1007/s10517-008-0084-8

Key Words

Search

Navigation