- The preparation and characterisation of cyclam/anthraquinone macrocyle/intercalator complexes and their interactions with DNA
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A new series of macrocycle/intercalator adducts have been prepared from cyclam (1,4,8,11-tetraazacyclotetradecane) and the 1- and 2-substituted anthraquinones (1-[(2-aminoethyl)amino]anthracene-9,10-dione (1C2mac), 1-[(3-amino-propyl)amino]anthracene-9,10-dione (1C3mac), 2-[(3-aminopropyl)amino]anthracene-9,10-dione (2C3mac)). The copper complexes of two of these adducts were prepared and the crystal structure of the complex of 1C2mac ([Cu(1C2mac)(CH3CN)2](PF6)2.0.2H 2O) was determined as the hexafluorophosphate salt. The equilibrium constants for the binding to DNA of 1C2-mac, with and without the copper added, were found by UV titrations to be 4.7 × 103 M-1 and 6.2 × 103 M-1, respectively. Reaction with plasmid DNA allowed comparison between the effects of the cyclam/anthraquinone adducts, their copper complexes and the intercalators alone. Addition of the macrocycle increased the extent and effect of DNA intercalation and addition of copper increased the effect still further. The adducts with the longer side chains caused substantially more unwinding of the DNA. None of the adducts inhibited cleavage at dGpG or dGpC sites by restriction enzymes. Molecular modelling was used to investigate the effects of the side chain for a number of possible DNA binding modes. These models reveal that intercalation is not significantly interfered with by the presence of the macrocycle, irrespective of the position of attachment. The increased unwinding caused by adducts with the longer side chain is therefore most likely to be due to specific interactions between the macrocycle and the DNA.
- Ellis, Leanne T.,Perkins, David F.,Turner, Peter,Hambley, Trevor W.
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- NOVEL CHROMOPHORIC SILYL PROTECTING GROUPS AND THEIR USE IN THE CHEMICAL SYNTHESIS OF OLIGONUCLEOTIDES
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The present invention provides compounds of the formula (I): C-Q-O-Si (R1)(R2)-N wherein C is a chromophore; Q is selected from the group consisting of optionally substituted aliphatic, aryl, heteroaryl, cycloalkyl or heterocycloalkyl; R1 and R2 are independently selected from the group consisting of optionally substituted C1-8 alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, C1-8 alkyloxy, cycloalkyloxy, heterocycloalkyloxy, alkylsilyloxy and arylsilyloxy; and N is a glycosylamine or abasic moiety.
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Page/Page column 20; sheet 7
(2009/01/20)
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- COLOURED SILSESQUIOXANES
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The invention relates tp dye-functionalized silsesquioxane clusters, a process for their manufature and their use as colorants, wherein the compounds (functionalized clusters or nano-particles) are characterized by the general formula (I) wherein CAGE is a moiety of the formula (IA) D is a chromophoric moiety, and the other symbols have the meanings as defined in the specification, or salts thereof.
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Page/Page column 25-26
(2008/06/13)
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- Anti-cancer agents
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A compound is provided having the formula: wherein R1 and R2 are independently hydrogen, hydroxy, alkoxy or acyloxy R3 and R4 are independently oxo, hydroxy or hydrogen; one of R5 or R6 is -A-B and the other is hydrogen, hydroxy, alkoxy, acyloxy, a group -A-B or a group -amino-R7—O—Y; the or each A is independently a spacer group having the formula -amino-R7—O— which is bonded to the anthracene ring via the amino group nitrogen and to B via the —O— atom R7 is a divalent organic radical; B is an amino acid residue, a peptide group, or isostere thereof; and Y is hydrogen or a capping group, or a physiologically acceptable derivative thereof. The compounds primarily have utility against cancers, but also have use against viruses and parasites having topoisomerases.
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- Aza-Crown Ethers with Quinone Side Chains: Synthesis, Complexation, and Protonation
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The synthesis and spectroscopic investigation of aza-crown ethers with anthraquinone- and 1-aminoanthraquinone-functionalized side chains are described.Cation-induced shifts in the UV/VIS absorption spectra of the ligands dissolved in propylene carbonate are observed only for Li+ among the alkali metal ions and for Mg2+ among the alkaline earth metal ions as well as for Ag+ and Tl+.Only hypsochromic shifts of the absorption spectra of anthraquinone-bearing aza-crown ethers are observed on protonation.The variations of the extinction coefficients are discussed with respect to the sequence of protonation of the different amino groups.
- Ossowski, Tadeusz,Schneider, Hermann
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p. 1673 - 1677
(2007/10/02)
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- Anormalous Halogen to Dimethylamino Replacement with N,N-Dimethylformamide Catalyzed by Ethylenediamine or 2-Aminoethanol
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1- And 2-chloroanthraquinone and 2-amino-4-chloro-6-hydroxypyrimidine exclusively gave the dimethylamino derivatives upon heating in DMF at 90 deg C in the presence of ethylenediamine or ethanolamine.A possible reaction pathway for this unusual exchange reaction was discussed.
- Yamamoto, Hiroshi
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p. 2685 - 2686
(2007/10/02)
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