Abstract
Three groups of distamycin analogues containing benzene units, potential minor groove binders, each containing six compounds, have been synthesized using Syncore Reactor. Ethidium bromide assay was used to show that these compounds bind to plasmid pBR322. The most active in fluorescence reduction appeared to be compounds with configuration meta-meta of benzene rings, formed library D.
Keywords: Combinatorial chemistry, Distamycin analogues, DNA binding, Parallel synthesis, Solid phase synthesis, meta-meta, benzene rings, DNA, helical curve, B-DNA, distamycin, Streptomyces distallicus, nitroamines, solid-phase syntheses, Ethidium bromide displacement assay
Letters in Drug Design & Discovery
Title: Semi-Automatic Synthesis of Distamycin Analogues and their DNA Binding Properties
Volume: 9 Issue: 1
Author(s): Danuta Drozdowska and Jakub Szerszenowicz
Affiliation:
Keywords: Combinatorial chemistry, Distamycin analogues, DNA binding, Parallel synthesis, Solid phase synthesis, meta-meta, benzene rings, DNA, helical curve, B-DNA, distamycin, Streptomyces distallicus, nitroamines, solid-phase syntheses, Ethidium bromide displacement assay
Abstract: Three groups of distamycin analogues containing benzene units, potential minor groove binders, each containing six compounds, have been synthesized using Syncore Reactor. Ethidium bromide assay was used to show that these compounds bind to plasmid pBR322. The most active in fluorescence reduction appeared to be compounds with configuration meta-meta of benzene rings, formed library D.
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Drozdowska Danuta and Szerszenowicz Jakub, Semi-Automatic Synthesis of Distamycin Analogues and their DNA Binding Properties, Letters in Drug Design & Discovery 2012; 9 (1) . https://dx.doi.org/10.2174/157018012798192919
DOI https://dx.doi.org/10.2174/157018012798192919 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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