AI Article Synopsis
- - Arterial thrombosis poses significant risks for cancer patients and can negatively impact their prognosis, prompting research into potential treatments involving P-selectin inhibition and DNA intercalation.
- - The study developed and tested 12 derivatives of bisindole-2-carboxylic acids, ultimately focusing on a compound named DEBIC, which showed anti-tumor effects by intercalating DNA and selectively inhibiting tumor cell growth.
- - DEBIC demonstrated the ability to slow tumor growth in mouse models and effectively inhibited arterial thrombosis by downregulating P-selectin at low doses.
Article Abstract
Arterial thrombosis is one of the major complications of cancer and can seriously worsen the prognosis of the patients. These clinical findings encouraged this paper to correlate P-selectin inhibition and DNA intercalation in cancer therapy and complicated thrombosis. By designing and docking 12 derivatives of bisindole- 2-carboxylic acids into the active sites of P-selectin and d(CGATCG) 9 derivatives were assigned to receive anti-tumor assay, and finally provided dimethyl 2,2'-[(2,2'-(ethane-1,1-diyl)bis(1-indole-3,2-diyl)]diacetate (DEBIC) to receive assays. DEBIC intercalated DNA and inhibited proliferation of tumor cells but not non-tumor cells. It slowed tumor growth of S180 mice at a dose of 0.36 μmol/kg, and slowed tumor growth of A549 bearing BABL/C mice at a dose of 8.9 μmol/kg. DEBIC was also found to inhibit arterial thrombosis by down regulating P-selectin effectively at a dose of 0.36 μmol/kg.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6114953 | PMC |
| http://dx.doi.org/10.18632/oncotarget.23151 | DOI Listing |
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