Photoinduced cleavage of DNA by bromofluoroacetophenone-pyrrolecarboxamide conjugates.

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.

journal_name

Bioorg Med Chem Lett

authors

Wender PA,Jeon R

doi

10.1016/s0960-894x(03)00212-9

subject

Has Abstract

pub_date

2003-05-19 00:00:00

pages

1763-6

issue

10

eissn

0960-894X

issn

1464-3405

pii

S0960894X03002129

journal_volume

13

pub_type

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