Abstract
A series of novel substituted acridones (1–15) have been synthesized. Their in vitro cytotoxicity against human breast adenocarcinoma (MCF-7) and human promyelocytic leukemia (HL-60) cell lines has been investigated. The compounds 11, 12, 14 and 15 showed moderate activity against MCF-7 cell lines with IC50 value < 5.83 μM. The compounds 8, 10–12, and 15 showed moderate activity against HL-60 cell lines with IC50 value < 1.75 μM. The DNAbinding properties of the compounds were evaluated based on their affinity or intercalation with CT-DNA measured with absorption titration. The compound 12 bearing planar diacetoxy tricyclic ring linked with butyl piperidine side chain showed highest binding affinity with binding constant (Ki) 10.38 ×10 ×M–1. The examination of the relationship between lipophilicity and cytotoxic properties of acridones showed a poor correlation.
Highlights
Cytotoxic drugs remain the mainstay of cancer chemotherapy and are being administered with novel ways of therapy such as inhibitors of signals
In the view of above literature, we have designed 1,3-diacetoxyacridone ring nucleus substituted at N10-position with propyl and butyl side chains followed by tertiary amino groups for better cytotoxicity and DNA-binding properties (1–15, Tab. 1)
The cytotoxicity of fifteen compounds was examined on MCF-7 and HL-60 cell lines by Trypan blue exclusion method with several concentrations of acridones
Summary
Cytotoxic drugs remain the mainstay of cancer chemotherapy and are being administered with novel ways of therapy such as inhibitors of signals. In the view of above literature, we have designed 1,3-diacetoxyacridone ring nucleus substituted at N10-position with propyl and butyl side chains followed by tertiary amino groups for better cytotoxicity and DNA-binding properties (1–15, Tab. 1). Has been tested against MCF-7 and HL-60 cell lines and tried to correlate the lipophilicity, DNA-binding properties with cytotoxicity.
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