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Photoinduced cleavage of DNA by bromofluoroacetophenone-pyrrolecarboxamide conjugates
- Authors
- Wender, PA; Jeon, R
- Issue Date
- May-2003
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.13, no.10, pp 1763 - 1766
- Pages
- 4
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Volume
- 13
- Number
- 10
- Start Page
- 1763
- End Page
- 1766
- ISSN
- 0960-894X
1464-3405
- Abstract
- Bromofluoroacetophenone derivatives which produce fluorine substituted phenyl radicals that cleave DNA upon excitation were investigated as a novel photonuclease. Pyrrolecarboxamide-conjugated bromofluoroacetophenones; 4'-bromo-2'-fluoroacetophenone and 2'-bromo-4'-fluoroacetophenone were synthesized and their DNA cleaving activities and sequence selectivities were determined. Bromofluoroacetophenone-pyrrolecarboxamide conjugates were. found to be effective DNA cleaving agents upon irradiation in concentration dependent manner based on plasma relaxation assay. The DNA cleaving activities of 2'-bromo-4'-fluoroacetophenone derivatives were larger than those of 4'-bromo-2'-fluoroacetophenone derivatives. (C) 2003 Elsevier Science Ltd. All rights reserved.
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