Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2013 Jun 1;23(11):3277-82.
doi: 10.1016/j.bmcl.2013.03.110. Epub 2013 Apr 8.

Antiproliferative activity of 2,3-disubstituted indoles toward apoptosis-resistant cancers cells

Igor V Magedov  1 , Florence Lefranc, Liliya V Frolova, Laetitia Moreno Y Banuls, Amanda S Peretti, Snezna Rogelj, Véronique Mathieu, Robert Kiss, Alexander Kornienko
Affiliations

Antiproliferative activity of 2,3-disubstituted indoles toward apoptosis-resistant cancers cells

Igor V Magedov et al. Bioorg Med Chem Lett. .

Abstract

Many types of cancer, including glioma, melanoma, NSCLC, among others, are resistant to apoptosis induction and poorly responsive to current therapies with propaptotic agents. We describe a series of 2,3-disubstituted indoles, which display cytostatic rather than cytotoxic effects in cancer cells, and serve as a new chemical scaffold to develop anticancer agents capable of combating apoptosis-resistant cancers associated with dismal prognoses.

PubMed Disclaimer

Figures

Figure 1
Figure 1
Cellular imaging of B10 against melanoma SKMEL-28 and NSCLC A549 cells illustrating non-cytotoxic, but cytostatic, antiproliferative mechanism at MTT colorimetric assay-related GI50 concentrations after 72 h of cell culture with the drug.
Figure 2
Figure 2
Percentage of cells that lost plasma membrane integrity after treatment with B10 as assessed by propidium iodide staining. Positive controls correspond to fixed and permeabilized corresponding cells.
Scheme 1
Scheme 1
Scheme 2
Scheme 2
See this image and copyright information in PMC

Similar articles

See all similar articles

Cited by

References

    1. Brenner H. The Lancet. 2002;360:1131. - PubMed
    1. Kleihues P, Cavenee WK. Pathology and Genetics of Tumors of the Nervous System, International Agency for the Research on Cancer (IARC) and WHO Health Organization. Oxford, UK: Oxford Press; 2000.
    1. Lefranc F, Sadeghi N, Camby I, Metens T, De Witte O, Kiss R. Expert Rev. Anticancer Ther. 2006;6:719. - PubMed
    1. Stupp R, Hegi ME, Mason WP, van den Bent MJ, Taphoorn MJ, Janzer RC, Ludwin SK, Allgeier A, Fisher B, Belanger K, et al. Lancet Oncol. 2009;10:459. - PubMed
    1. Giese A, Bjerkvig R, Berens ME, Westphal M. J. Clin. Oncol. 2003;21:1624. - PubMed

Publication types