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  • 1980-1984  (3)
  • 1975-1979  (2)
  • 1
    Electronic Resource
    Electronic Resource
    Influence of 4′-6-diamidino-2-phenylindole on the secondary structure and template activities of DNA and polydeoxynucleotides (1977)
    Springer
    Molecular and cellular biochemistry 18 (1977), S. 81-86 
    Details
    ISSN: 1573-4919
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology , Medicine
    Notes: Summary The interaction between 4′-6-Diamidino-2-Phenylindole-hydrochloride (DAPI) and a variety of DNAs and synthetic polydeoxynucleotides was investigated in order to delineate the nucleic acid structural features necessary for binding. The spectra of DAPI-DNA complexes, measured at various DAPI-DNA molar ratios (r), are hypochromic relative to DNA in the region of its maximum absorption. All the curves pass through an isosbestic point at 268 nm. A new maxima appears in the region of 380–392 nm for DAPI-DNA complexes. The magnitude of the peaks in the region are directly proportional to the amount of drug present in the complex. Studies with various DNA types and synthetic polydeoxynucleotides indicate that the drug preferentially binds to dAT-rich regions of DNA. This was also confirmed by enzymatic studies. The inhibition of template action by DAPI in a purified DNA-polymerase reaction was dependent on the dAT-content of the template. The implication of these data to explain a selective binding of DAPI to mitochondrial DNA have been discussed.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00280272
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  • 2
    Electronic Resource
    Electronic Resource
    Inhibitory activity of diarylamidine derivatives on murine leukemia L1210 cell growth (1983)
    Springer
    Investigational new drugs 1 (1983), S. 103-115 
    Details
    ISSN: 1573-0646
    Keywords: diarylamidines ; diarylimidazolines ; murine leukemia L1210 ; DNA synthesis
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary A series of 96 diarylamidine (and diarylimidazoline) derivatives were evaluated for their inhibitory effects on the growth and DNA synthesis of murine leukemia L1210 cells. The amidino- and imidazolino-substituted aryl moieties of the compounds consisted of phenyl, indole, indene, benzofuran, benzo[b]thiophene or benzimidazole. Several of these compounds were found to inhibit L1210 cell proliferation with an ID50 (50% inhibitory dose) of 1 μg/ml or lower. Structure-function analysis revealed that the antitumor cell activity of the diarylamidines depended on the planarity of the molecule, the presence of amidino- (or, preferably, imidazolino-) groups on both aryl moieties, the nature of the bridge connecting the two aryl moieties (preferably no bridge at all, phenoxy or ethene) and, finally, the nature of the aryl moieties (preferably, benzofuran or benzo[b]thiophene). Hence, compound 20 (6-(2-imidazolin-2-yl)-2-[4-(2-imidazolin-2-yl)phenyl] benzo[b]thiophene) emerged as the most potent inhibitor of L1210 cell growth (ID50: 0.21 μg/ml). Its inhibitory potency was similar to that of the well-known trypanocidal drug ethidium bromide (compound 98). For all diarylamidine derivatives taken together, some correlation (r = 0.612) was noted between the log ID50 for L1210 cell proliferation and the log ID50 for L1210 cell DNA synthesis (as monitored by [methyl 3H]dThd incorporation). These findings suggest that the inhibitory effects of the diarylamidines on L1210 cell proliferation may at least partially reside in an inhibition of DNA synthesis. Compound 41 (2,2′-vinylenedi-1-benzofuran-5-carboxamidine), that exhibited a potent antitumor activity in vitro (ID50: 1.5 μg/ml), was further evaluated for its antitumor efficacy in vivo and found to increase the median survival time of L1210 cell-inoculated BDF1 mice up to 204%, if administered at a dose of 200 mg/kg.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00172069
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  • 3
    Electronic Resource
    Electronic Resource
    Synthesen biskationischer, trypanocider 1-Benzofuran-Verbindungen (1982)
    Weinheim : Wiley-Blackwell
    Liebigs Annalen 1982 (1982), S. 1836-1869 
    Details
    ISSN: 0170-2041
    Keywords: Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Syntheses of Biscationic, Trypanocidal 1-Benzofuran Compounds2-Phenyl-1-benzofurans with the substituents Br, NO2, CN, and -NH2, -NH-C(=NH)-NH2, -C(=NH)-NH2, -C=N-CH2-CH2-NH in 4′,5-position were synthesized.  -  For arylated formamidine derivatives [Ar-N=CH-N(CH3)2] a simple new preparation was found by reacting amine hydrochlorides with dimethylformamide in the presence of cyanamide.  -  Based on 5- or 6-cyano-1-benzofuran-2-carboxylates a series of α,ω-bis(1-benzofuran-2-yl) derivatives with cyano-, amidino-, or imidazolinyl groups in 5- or 6-position was prepared.
    Notes: 2-Phenyl-1-benzofurane mit den Substituenten Br, NO2 sowie CN und -NH2, -NH-C(=NH)-NH2, -C(=NH)-NH2 sowie -C=N-CH2-CH2-NH in 4′,5-Stellung wurden synthetisiert.  -  Für arylierte Formamidin-Derivate [Ar-N=CH-(CH3)2] fand sich in der Umsetzung von Aminhydrochloriden mit Dimethylformamid in Gegenwart von Cyanamid ein einfaches, neues Herstellungsverfahren.  -  Auf der Basis von 5- oder 6-Cyan-1-benzofuran-2-carbonsäureester konnte eine Serie von α,ω-Bis(1-benzofuran-2-yl)-Derivaten mit Cyan- oder Amidino- oder Imidazolinyl-Gruppen in 5- oder 6-Stellung dargestellt werden.
    Additional Material: 4 Tab.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/jlac.198219821008
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  • 4
    Electronic Resource
    Electronic Resource
    Synthesen antimikrobieller biskationischer 2-(Phenoxyphenyl)-indole und -1-benzofurane (1984)
    Weinheim : Wiley-Blackwell
    Liebigs Annalen 1984 (1984), S. 409-425 
    Details
    ISSN: 0170-2041
    Keywords: Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Syntheses of Antimicrobial Biscationic 2-(Phenoxyphenyl)indoles and -1-benzofuransTen 2-(phenoxyphenyl)indoles and four 2-(phenoxyphenyl)-1-benzofurans with terminal amidinium or imidazolinium groups were synthesized in respect to growth inhibiting properties.
    Notes: Zehn 2-(phenoxyphenyl)indole und vier 2-(Phenoxyphenyl)-1-benzofurane mit endständigen Amidinium- oder Imidazolinium-Gruppen wurden im Hinblick auf wachstumshemmende Eigenschaften synthetisiert.
    Additional Material: 2 Tab.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/jlac.198419840302
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  • 5
    Electronic Resource
    Electronic Resource
    Trypanocide Diamidine mit drei isolierten Ringsystemen (1975)
    Weinheim : Wiley-Blackwell
    Liebigs Annalen 1975 (1975), S. 160-194 
    Details
    ISSN: 0075-4617
    Keywords: Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Trypanocidal Diamidines with Three Isolated Ring SystemsA benzene ring added to the five membered ring of diamidines of type A diminishes the trypanocidal properties, as shown by the examples 3e, 4d and 5d having the skeleton of 2,3-diphenylbenzo[b]thiophene and of 2,3-diphenylindole, without gain of bacteriostatic or fungistatic properties. Such a gain can be achieved by insertion of a phenoxy grouping as shown by the diamidines 7b and 7c of indole substituted by -C6H4-X-C6H4-R (X = 0 or OCH2-CH20). They were synthesized by condensing substituted o-nitrophenylacetic acid with phenol or ethers thereof in hydrogen fluoride to yield 2'-nitrodeoxybenzoins, which on reduction with zinc dust in acetic acid led to indoles; reduction with fresh iron(I1) hydroxide afforded 3H-indoles. - If the five membered ring of type A is no longer fused to the benzene ring diamidines with the three-membered skeleton, benzene-hetereocyclic five-membered ring-benzene, are obtained which only retain activity against Trypanosoma rhodesiense. This activity is exeedingly high for the isoxazole 45c.
    Notes: Ein zusätzlicher Benzolring am Fünfring von Diamidinen des Typs A vermindert die trypanocide Eigenschaft, wie sich an Beispielen mit dem Gerüst des 2,3-Diphenylbenzo[b]-thiophens (3e) und des 2,3-Diphenylindols (4d, 5d) zeigt, ohne Gewinn an bakteriostatischen oder fungistatischen Eigenschaften. Dieser Gewinn kann durch eine „Phenoxyerweiterung“ erzielt werden, wie sich an den in 2-Stellung durch -C6H4-X-C6H4-R (X = 0 oder OCH2-CH20) substituierten Diamidinen 7b und 7c des Indols zeigt. Zu ihrer Synthese wurden substituierte o-Nitrophenylessigsäuren mit Phenol oder Phenoläthern in Fluorwasserstoff zu 2'-Nitrodesoxybenzoinen kondensiert, bei deren Reduktion mit Zinkstaub in Eisessig Indolverbindungen entstanden, während eine Reduktion mit frischem Eisen(I1)-hydroxid zu 3H-Indolverbindungen führte. - Eine Aufhebung der Anellierung des Fünfringes beim Typ A bewahrt bei Diamidinen mit dem dreiteiligen Ger¨ust, Benzol-hetereocyclischer Fünfring-Benzol, nurmehr eine Wirksamkeit gegen Trypanosoma rhodesiense, welche bei dem Isoxazol 45c überragend ist.
    Additional Material: 1 Tab.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/jlac.197519750115
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