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. 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.

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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

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