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  • 1980-1984  (3)
  • 1970-1974  (6)
  • 1
    Electronic Resource
    Electronic Resource
    Chromane, XVIII Synthese von 7α-Methyl-6-oxa-östron (1971)
    Weinheim : Wiley-Blackwell
    Berichte der deutschen chemischen Gesellschaft 104 (1971), S. 3313-3328 
    Details
    ISSN: 0009-2940
    Keywords: Chemistry ; Inorganic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Chromanes, XVIII Synthesis of 7α-Methyl-6-oxaestroneReaction of 7-methoxy-2-methyl-4-oxochromane with vinylmagnesium bromide and then with 2-methyl-1.3-dioxocyclopentane resulted in the formation of 3-methoxy-7-methyl-17-oxo-6-oxaestra-1.3.5(10).8.14-pentaene (4b). Its catalytic hydrogenation led solely to the C//D-cis compounds 5 and 6. Only after hydrogenation of the 17-oxo group in 4b with sodium boron hydride to 8b did the catalytic hydrogenation yield the C//D-trans series 9b→10b→11b→7α-methyl-6-oxaestrone methyl ether (12b). An analogous sequence beginning with the tetrahydropyranyl ether 4c led via 8c→9c→10c→11a to 7α-methyl-6-oxaestrone (12a).
    Notes: Umsetzung von 7-Methoxy-2-methyl-chromanon-(4) mit Vinylmagnesiumbromid und dann mit 2-Methyl-cyclopentandion-(1.3) gab 3-Methoxy-7-methyl-6-oxa-östrapentaen-(1.3.5(10).8.14)-on-(17) (4b). Dessen katalytische Hydrierung ergab nur die C//D-cis-verknüpften Verbindungen 5 und 6. Erst nach Natriumborhydrid-Reduktion der 17-Ketogruppe in 4b zu 8b führte die katalytische Hydrierung in die C/D-trans-verknüpfte Reihe 9b→10b→11b→7α-Methyl-6-oxa-östron-methyläther (12b). Eine analoge Reaktionsfolge mit dem Tetrahydropyranyläther 4c lieferte auf dem Wege 8c→9c→10c→11a 7α-Methyl-6-oxa-östron (12a).
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/cber.19711041035
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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
    Mehrkernige Thiophene, VIII1) Trypanocide Diamidine des 2-Phenyl-thionaphthens (1970)
    Weinheim : Wiley-Blackwell
    Liebigs Annalen 734 (1970), S. 23-45 
    Details
    ISSN: 0075-4617
    Keywords: Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Polynuclear Thiophenes, VIII1). Trypanocidal Diamidines of 2-Phenyl-thionaphtheneThe diamidines of 2-phenyl-thionaphthene with the amidino groups in the positions 4′, 6 (7), 4′,5 (19e), 3′.6 (12g) and 3′,5 (14g) are synthesized. The 1.1-dioxides 20b and 22b of the 4′,6-and of the 4′,5-diamidines are also prepared as well as the corresponding 1,1-dioxides hydrogenated in 2,3-position (21b, 23b). - Both the 4′,6- and the 4′,5-diamidine exhibit in mice a general and outstanding trypanocidal activity which culminates for the 4′,6-compound 7 in the highest activity against T. gambiense.
    Notes: Die Diamidine des 2-Phenyl-thionaphthens mit den Amidinogruppen in 4′.6-(7), 4′.5-(19e), 3′.6-(12g) und 3′.5-Stellung (14g) werden synthetisiert. Vom 4′.6- und vom 4′.5-Diamidin werden die 1.1-Dioxide (20b, 22b) sowie deren 2.3-Dihydro-Derivate (21b, 23b) hergestellt. - Das 4′.6- und das 4′.5-Diamidin zeigen im Mäuseversuch ein ausgezeichnetes trypanocides Wirkungsspektrum (Tab. 1), worin die 4′.6-Verbindung 7 die höchste Wirksamkeit gegen T. gambiense aufweist.
    Additional Material: 3 Tab.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/jlac.19707340104
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  • 6
    Electronic Resource
    Electronic Resource
    Trypanocide Diamidine mit vier Ringen in einem oder zwei Ringsystemen (1973)
    Weinheim : Wiley-Blackwell
    Liebigs Annalen 1973 (1973), S. 1112-1140 
    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 Four Rings in One or Two Ring SystemsThe trypanocidal properties of diamidines of type A are diminished by rigidity of the skeleton and by its enlargement, as was shown by preparation of diamidines with the following skeletons: 10H-[1]benzothieno[3,2-b]indole (1c); chrysene (4g); cis-4b,5,6,10b,11,12-hexa-hydrochrysene (8g); 2-(2-benzofuranyl)indole (10c, 11c); 2-naphthylbenzo[b]thiophene (12d), 1-phenylnaphtho[2,1-b]thiophene (18c); bis(2-benzofuranyl)-methane (24d), -ethylenes (25c, 28c, 31c) and -ethanes (29b, 30b).
    Notes: Die trypanociden Eigenschaften der Diamidine vom Typ A werden durch Starrheit des Molekülgerüstes und durch seine Flächenvergrößerung beeinträchtigt, wie sich durch die Darstellung von Diamidinen mit folgenden Gerüsten zeigen ließ: 10H-[1]Benzothieno-[3,2-b]indol (1c); Chrysen (4g); cis-4b,5,6,10b,11,12-Hexahydrochrysen (8g); 2-(2-Benzofuranyl)indol (10c, 11c); 2-Naphthylbenzo[b]thiophen (12d); 1-Phenylnaphtho[2,1-b]thiophen (18c); Bis(2-benzofuranyl)-methan (24d), -äthylene (25c, 28c, 31c) und -äthane (29b, 30b).
    Additional Material: 1 Tab.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/jlac.197319730708
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  • 7
    Electronic Resource
    Electronic Resource
    Gegen Malaria wirksame 6-Aminochinoline, II. 6-[ω-Diäthylamino-alkylamino]- und 6-[ω-Amino-alkylamino]-5.8-dimethoxy-chinaldine (1971)
    Weinheim : Wiley-Blackwell
    Liebigs Annalen 744 (1971), S. 119-128 
    Details
    ISSN: 0075-4617
    Keywords: Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Antimalarial 6-Aminoquinolines, II. 6-[ω-Diethylaminoalkylamino]- and 6-[ω-Aminoalkyl-amino]-5,8-dimethoxyquinaldinesTwelve derivatives of 6-amino-5,8-dimethoxyquinaldine with the basic side chains (C2H5)2N—(CH2)n—NH (n = 2, 3; 15, 16) and H2N—(CH2)n—CHR—NH— (n = 1 - 9, R = H, CH3; 21a-k) in the 6-position are prepared with the aim of studying the influence of the basic side chain on malarial activity and toxicity of the 6-aminoquinolines.
    Notes: Zwölf in 6-Stellung basisch alkylierte 6-Amino-5.8-dimethoxy-chinaldine mit den Seiten-ketten (C2H5)2N—(CH2)n—NH— (n = 2, 3; 15, 16) und H2N—(CH2)n—CHR—NH—(n = 1—9, R = H, CH3; 21a-k) wurden synthetisiert, um den Einfluß der basischen Seitenkette auf Malaria-Wirksamkeit und Toxizität der 6-Amino-chinoline zu untersuchen.
    Additional Material: 3 Tab.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/jlac.19717440115
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  • 8
    Electronic Resource
    Electronic Resource
    Trypanocide Diamidine des 2-Phenyl-benzofurans, 2-Phenyl-indens und 2-Phenyl-indols (1971)
    Weinheim : Wiley-Blackwell
    Liebigs Annalen 749 (1971), S. 68-89 
    Details
    ISSN: 0075-4617
    Keywords: Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Trypanocide Diamidines of 2-Phenylbenzofuran, 2-Phenylindene and 2-PhenylindoleDiamidines with the amidino-groups in 4′.5- and 4′.6-position of the ring skeletons of 2-phenylbenzofuran (4e, 5e, 3e), of 2-phenylindene (10d, 16a, 16b, 16c, 16d), of 2-phenyl-2.3-dihydroindene (17b) and of 2-phenylindole (18l, 18n, 18p, 19d, 19e) are synthesized; the 3′.5- and 3′.6-diamidines 18m, 18o of 2-phenylindole are also prepared. - The activity of 4′.5-diamidine 4e of 2-phenylbenzofuran against Trypanosoma rhodesiense surpasses all others. The spectrum of activity of diamidines of 2-phenylindene resembles that of the diamidines of 2-phenylthionaphthene with the main activity against T. gambiense. The 4′.6-diamidine 18n of 2-phenylindole exhibits the highest and rarely found activity against T. congolense.
    Notes: Es werden Diamidine synthetisiert, welche die Amidino-Gruppen in 4′.5- bzw. 4′.6-Stellung der Ringgerüste des 2-Phenyl-benzofurans (4e, 5e und 3e), des 2-Phenyl-indens (10d, 16a, 16b, 16c, 16d), des 2-Phenyl-2.3-dihydro-indens (17b) sowie des 2-Phenyl-indols (18l, 18n, 18p, 19d, 19e) enthalten; von letzterem werden außerdem die 3′.5- bzw. 3′.6-Diamidine (18m bzw. 18o) dargestellt. - Das 4′.5-Diamidin 4e des 2-Phenyl-benzofurans besitzt eine überragende Wirksamkeit gegen Trypanosoma rhodesiense. Die Diamidine des 2-Phenylindens haben ein Wirkungsspektrum wie jene des 2-Phenyl-thionaphthens mit dem Schwerpunkt gegen T. gambiense, und das 4′.6-Diamidin 18n des 2-Phenyl-indols besitzt eine überragende, seltene Wirksamkeit gegen T. congolense.
    Additional Material: 5 Tab.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/jlac.19717490110
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  • 9
    Electronic Resource
    Electronic Resource
    Trypanocide Diamidine mit drei Ringen in zwei isolierten Ringsystemen (1972)
    Weinheim : Wiley-Blackwell
    Liebigs Annalen 760 (1972), S. 37-87 
    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 Rings in Two Isolated Ring SystemsDiamidines are synthesized, which are derived of type A of 6- or 5-amidino-2-[4-amidino-phenyl]-thionaphthene or -benzofuran by further variation of the condensed five-membered ring, by insertion of a bridge of one or two atoms between the two ring systems and by variation of the amidino groups. - Only 5-amidino-2-[4-amidinophenyl]-indazole (4c) and -benztriazole (10d) retained the outstanding trypanocidal properties of type A.
    Notes: Es werden Diamidine synthetisiert, welche sich vom Typ A des 6- oder 5-Amidino-2-[4-amidino-phenyl]-thionaphthens oder -benzofurans dadurch ableiten, daß der annelierte Fünfring weiter variiert wird, daß ein- und zweigliedrige Brücken zwischen die beiden Ringsysteme eingeschoben werden, und daß die flankierenden Amidino-Gruppen abgewandelt werden. - Nur bei 5-Amidino-2-[4-amidino-phenyl]-indazol (4c) und -benztriazol (10d) bleiben die hervorragenden trypanociden Eigenschaften des Typs A erhalten.
    Additional Material: 1 Tab.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/jlac.19727600105
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