Journal
MOLECULAR AND CELLULAR BIOCHEMISTRY
Volume 398, Issue 1-2, Pages 21-30Publisher
SPRINGER
DOI: 10.1007/s11010-014-2201-5
Keywords
Rhenium; DNA; X-ray Crytallography; Intercalation; Electronic spectroscopy; Brain cancer
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Funding
- Burroughs Wellcome Fund
- US-NIH-RISE
- US-National Science Foundation LSAMP institutional support Award
- TMCF-DOE award
- Department of Defense [W911NF-11-1-0157]
- National Institutes of Health [5G11HD038439]
- Nuclear Regulatory Commission [NRC-HQ-12-G-27-0086]
- U.S. Department of Energy, Office of Energy Sciences Materials Sciences Division [DEAC02-05CH11231]
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Seven organorhenium pentylcarbonate compounds (PC1-PC7) have been synthesized. DNA-binding studies of the PC-series compounds using electronic spectroscopy and gel electrophoresis suggest that the compounds presumably bind to DNA in an intercalative mode. The intrinsic binding constants for PC4, PC6, and PC7 were found to be 1.6 x 10(4), 3.9 x 10(4), and 4.2 x 10(4) M-1, respectively. The X-ray structure determinations and density functional theory calculations indicate that the polypyridyl ligands in the compounds are nearly planar facilitating DNA binding through an intercalation mechanism. Cytotoxicity studies of 10 A mu M pentylcarbonate compounds against HTB-12 human astrocytoma brain cancer cells were studied for 48 h. It was observed that each of the pentylcarbonate compounds is active against the cancer cells. However, under analogous conditions, CRL-2005 rat astrocyte normal brain cells are not affected significantly.
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