- Design, synthesis, and evaluation of phenanthridine derivatives targeting the telomerase RNA/DNA heteroduplex
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We are targeting molecules to the RNA/DNA heteroduplex that forms during the enzyme telomerase's catalytic cycle. Telomerase is a potential universal anti-cancer target that we have previously shown can be inhibited by molecules that target this heteroduplex. The aim of this work was to make derivatives of our lead, ethidium, that would allow its straightforward incorporation into molecules in both solid and solution phase. The heteroduplex targeting intercalator will act as a scaffold to allow the incorporation of new functionalities that will interact with specific protein surfaces of telomerase, thereby potentially increasing affinity and specificity. In examining multiple new derivatives of ethidium, with literature precedent or novel, we have identified one, a 5-benzylic acid ethidium derivative that is synthesized in three steps as a single isomer, and completely retains the inhibition efficacy of the parent compound. Furthermore, we have demonstrated that it can be effectively incorporated into resin bound amines on the solid phase. As such it represents an ideal monomer for the exploration of telomerse inhibition or for other applications which would benefit from hybrid molecules that can target duplexes.
- Rangarajan, Subhashree,Friedman, Simon H.
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- Fluorescent dye and preparation method and application thereof in bacterium detection
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The invention relates to a preparation method of a fluorescent dye. The fluorescent dye can be applied to bacterium detection. The fluorescent dye disclosed by the invention is combined with a photoreactive dye of dsDNA in virtue of high affinity; the self-fluorescence of the fluorescent dye is very weak, but however, a strong fluorescence signal is obtained after bonding of the fluorescent dye with nucleic acid; the fluorescent dye is impermeable to cell membranes and can only enter damaged cell membranes for bonding to DNAs through covalent bonds, so permanent DNA modification is realized; and the modified DNAs cannot be amplified again, so the defects of conventional detection methods can be well overcome when the fluorescent dye is used in cooperation with a PCR method.
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Paragraph 0045-0047
(2019/12/27)
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- A novel nucleic acid dye preparation and application thereof
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The present invention discloses a novel nucleic acid dye having the following structure general formula. According to the present invention, in the case of maintaining of high sensitivity and high stability of the excellent nucleic acid dye and compatibility with the existing detection instrument, the molecular structure is improved so as to easily penetrate into the high intensity polymer such as polyacrylamide gel, wherein the original nucleic acid dye molecules are the macromolecular structure while the products included in the present invention are the small molecular structure, such that the technical difficulty that the fluorescent dye adopted as the nucleic acid gel dye difficultly penetrates into the nucleic acid to cause the poor dyeing effect is solved; and the molecular structure is improved to increase the amount of the charge carried by the product, such that the dye can not penetrate into the cell membrane and the high safety standard is achieved so as to solve the high toxicity problem of the general nucleic acid dye .
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Paragraph 0098; 0099; 0100; 0101; 0102; 0103; 0104;
(2017/07/31)
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- Improvement of ways to obtain ethidium bromide and synthesis of ethidium ethyl sulfate, a new fluorescent dye for detection of nucleic acids
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Two methods for synthesis of ethidium bromide, a fluorescent dye widely used in molecular biology, were improved. An analog of ethidium bromide, ethidium ethyl sulfate, was synthesized.
- Osadchii,Shubin,Kozlova,Varlamenko,Filipenko,Boyarskikh
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p. 1541 - 1548
(2012/01/14)
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- SYNTHESE DANS LA CHIMIE DES PHENANTHRIDINES. III. PREPARATION DE QUELQUES MODELES D'ACIDES ω-(DIAMINO-3,8 PHENANTHRIDINYL-6) CARBOXYLIQUES
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New series of ω-(3,8-diamino-6-phenanthridinyl) alkanoic acids are obtained from the acid chloride-esters ROCO(CH2)nCOCl (n =0, 3 to 8; R = Me or Et).Reaction of these with 2-amino-3,8-dicarbethoxyaminobiphenyl leads to the expected 2-acylamino-3,8-dicarbethoxyaminobiphenyls which by cyclization lead to the corresponding methyl or ethyl (3,8-dicarbethoxyamino-6-phenanthridinyl)alkanoates.Quaternarization followed by hydrolysis has been performed to obtain some ω-(3,8-diamino-6-phenanthridinium) alkanoic acid salts.
- Lion, C.,Boukou-Poba, J. P.,Charvy, C.
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p. 171 - 181
(2007/10/02)
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