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Sci. Pharm. 2009, 77(1), 19-32; doi:10.3797/scipharm.0811-03

Synthesis of Novel 1,3-Diacetoxy-Acridones as Cytotoxic Agents and their DNA-Binding Studies

1
Medicinal Chemistry Research Division, V. L. College of Pharmacy, Raichur-584103, Karnataka, India
2
Acharya and BM Reddy College of Pharmacy, Bangalore, Karnataka, India
*
Author to whom correspondence should be addressed.
Received: 4 November 2008 / Accepted: 18 December 2008 / Published: 19 December 2008
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Abstract

A series of novel substituted acridones (115) 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, 1012, 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.
Keywords: 1,3-Diacetoxyacridone; Cytotoxicity; MCF-7; HL-60, DNA-binding; Calf-Thymus DNA 1,3-Diacetoxyacridone; Cytotoxicity; MCF-7; HL-60, DNA-binding; Calf-Thymus DNA
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

SATHISH, N.K.; RAJENDRA PRASAD, V.V.S.; RAGHAVENDRA, N.M.; SHANTA KUMAR, S.M.; MAYUR, Y.C. Synthesis of Novel 1,3-Diacetoxy-Acridones as Cytotoxic Agents and their DNA-Binding Studies. Sci. Pharm. 2009, 77, 19-32.

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