2. Academic Validation
  3. Cytotoxic activity of proflavine diureas: synthesis, antitumor, evaluation and DNA binding properties of 1',1''-(acridin-3,6-diyl)-3',3''-dialkyldiureas

Cytotoxic activity of proflavine diureas: synthesis, antitumor, evaluation and DNA binding properties of 1',1''-(acridin-3,6-diyl)-3',3''-dialkyldiureas

  • Bioorg Med Chem. 2008 Apr 1;16(7):3976-84. doi: 10.1016/j.bmc.2008.01.026.
Mária Kozurková 1,  Danica Sabolová,  Ladislav Janovec,  Jaromír Mikes,  Ján Koval',  Ján Ungvarský,  Miroslava Stefanisinová,  Peter Fedorocko,  Pavol Kristian,  Ján Imrich
Affiliations

Affiliation

  • 1 Department of Biochemistry, Institute of Chemistry, Faculty of Science, P. J. Safárik University, SK-04167 Kosice, Slovakia.
PMID: 18258438 DOI: 10.1016/j.bmc.2008.01.026
Abstract

The synthesis of novel 1',1''-(acridin-3,6-diyl)-3',3''-dialkyldiureas was reported. Their biological activity to inhibit cell proliferation was assessed by a MTT assay on two cell lines, HeLa and HCT-116, at micromolar concentration. 1',1''-(Acridin-3,6-diyl)-3',3''-dihexyldiurea hydrochloride was active on a HCT-116 cell line with an IC(50) value of 3.1 microM. The interaction of these compounds with calf thymus DNA was investigated by a variety of spectroscopic techniques including UV-vis, fluorescence and CD spectroscopy. From spectrofluorimetric titrations, binding constants for the DNA-drug complexes were determined (K=0.9-4.2x10(5) M(-1)). Antiproliferative activity of synthesized derivatives might be related to their intercalation into DNA.

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