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  • 1
    Electronic Resource
    Electronic Resource
    Indolo[2,1-a]isoquinolines. Syntheses, steroid hormone receptor binding affinities, and cytostatic activity (1990)
    s.l. : American Chemical Society
    Journal of medicinal chemistry 33 (1990), S. 153-160 
    Details
    ISSN: 1520-4804
    Source: ACS Legacy Archives
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1021/jm00163a026
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  • 2
    Electronic Resource
    Electronic Resource
    Synthesis of polymer electrolytes with high ion conductivity using experimental design of multicomponent polymer systems (1993)
    s.l. : American Chemical Society
    Industrial & engineering chemistry research 32 (1993), S. 3128-3134 
    Details
    ISSN: 1520-5045
    Source: ACS Legacy Archives
    Topics: Chemistry and Pharmacology , Process Engineering, Biotechnology, Nutrition Technology
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1021/ie00024a024
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  • 3
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    Unknown
    Kontinuät und Wandel in der sowjetischen Kafka-Rezeption (1990)
    Berlin : Periodicals Archive Online (PAO)
    Arcadia. 25:3 (1990) 304 
    Details
    ISSN: 0003-7982
    Topics: Linguistics and Literary Studies
    URL: http://gateway.proquest.com/openurl?url_ver=Z39.88-2004&res_dat=xri:pao:&rft_dat=xri:pao:article:d401-1990-025-03-000006
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  • 4
    Electronic Resource
    Electronic Resource
    Crystal structure and hormonal activity of 1,1-bis(4-hydroxyphenyl)-2-phenylethene (1993)
    Springer
    Monatshefte für Chemie 124 (1993), S. 1181-1193 
    Details
    ISSN: 1434-4475
    Keywords: 1,1-Bis(4-hydroxyphenyl)-2-phenylethene ; X-ray analysis ; Estrogenic and antiestrogenic activity ; Estrogen receptor affinity
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Zusammenfassung Es wurde eine komplette dreidimensionale Röntgenstrukturanalyse von 1,1-Bis(4-hydroxyphenyl)-2-phenylethen (BHPE) durchgeführt, wobei die Reflexe bei Raumtemperatur gesammelt wurden. Nach isotroper Verfeinerung derF-Werte ergab sich einR-Wert von 0.163.BHPE kristallisiert mit 8 Molekülen in einer Einheitszelle von monokliner Symmetrie mit Raumgruppe C2/c und den Zelldimensionena=20.851,b=15.505,c=10.536 Å, β=107.54°. DasBHPE-Molekül ist nicht flach. Die aromatischen Ringe sind aus der Ethen-Ebene mit Winkeln von −30.16° (Ring B), −51.45° (Ring C) und −33.49° (Ring A) herausgedreht. Der Bindungswinkel zwischen den 1,1-ständigen, 4-hydroxysubstituierten Phenylringen beträgt 115.3°, wobei dies einen Abstand von 9.636 Å für die Hydroxylgruppen ergibt. Es stellte sich heraus, daßBHPE ein „impeded“ Estrogen mit geringer antiestrogener Wirkung ist, obwohl seine Estrogen-Receptor-Affinität sehr hoch ist (29%, Estradiol 100%). Es wird der Einfluß der räumlichen Gegebenheiten inBHPE und verwandten Substanzen im Hinblick auf ihre estrogene/antiestrogene und Brustkrebs-hemmende Wirkung diskutiert.
    Notes: Summary A complete three-dimensional X-ray crystal structure analysis of 1,1-bis(4-hydroxyphenyl)-2-phenylethene (BHPE) has been carried out. Reflexes were collected at room temperature. After isotropic refinement ofF-values by least-squares,R is 0.163.BHPE crystallizes with 8 molecules in a unit cell of monoclinic symmetry, space group C2/c and cell dimensionsa=20.851,b=15.505,c=10.536 Å, β=107.54°. The molecule ofBHPE is not flat, the aromatic rings are twisted out of the ethene plane with angles of −30.16° (ring B), −51.45° (ring C) and −33.49° (ring A). The bond angle between the 1,1-standing, 4-hydroxy-substituted phenyl rings amounts to 115.3° resulting in a distance between the hydroxy groups of 9.636 Å.BHPE proved to be a weak “impeded” estrogen with minor antiestrogenic potency, though its estrogen receptor affinity is very high (29%, estradiol 100%). A discussion of the influence of the spatial structure ofBHPE and related substances on its estrogenic/antiestrogenic and mammary tumor-inhibiting potency is given.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00810027
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  • 5
    Electronic Resource
    Electronic Resource
    Effect of cisplatin on primary tumour growth and liver metastases in the M 5076 reticulum sarcoma: implication for new screening modalities (1993)
    Springer
    Journal of cancer research and clinical oncology 119 (1993), S. 312-314 
    Details
    ISSN: 1432-1335
    Keywords: Cisplatin ; M 5076 reticulum sarcoma ; Tumour growth ; Metastasis ; Screening model
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract We investigated the effect of cisplatin given at different treatment intervals on growth of the s.c.-implanted M 5076 reticulum sarcoma and the number of liver metastases at the end of the experiment (day 24). The later the treatment was started, the smaller was the tumour-inhibiting effect of cisplatin on primary tumour growth. Initiation of cisplatin treatment before day 14 after tumour implantation inhibited liver metastases completely. Treatment starting from day 14 or later did not influence the number of liver metastases. With regard to the clinical situation, the data imply that in the search for new leads in anticancer compounds, experimental conditions should concentrate on the inhibition of metastatic tumour growth.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01208835
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  • 6
    Electronic Resource
    Electronic Resource
    The EnDA endometrial adenocarcinoma: an oestrogen-sensitive, metastasizing, in vivo tumour model of the rat (1993)
    Springer
    Journal of cancer research and clinical oncology 119 (1993), S. 450-456 
    Details
    ISSN: 1432-1335
    Keywords: EnDA endometrial carcinoma ; Oestrogen sensitivity ; Tumour metastanses ; In vivo
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract A high percentage of endometrial carcinomas contain oestrogen and progesterone receptors. For endocrine therapy of recurrent endometrial carcinoma, only high-dose progestins are in clinical use. As, therefore, the development of new endocrine treatment strategies is of great interest, suitable animal models for this tumour are essential. Up to now, only human tumour xenografts transplanted in immune-deficient nude mice, but no syngeneic in vivo tumour models, have been available. In the present article we describe the hormone sensitivity of the EnDA endometrial adenocarcinoma of the DA/Han rat growing as s.c. implants in DA/Han rats and athymic nude mice in serial passage. In both species, the tumour expresses oestrogen, but no progesterone receptors. Transplanted in DA/Han rats or nude mice, ovariectomy reduced tumour weight by 64% and 46% respectively. In both species substitution of ovariectomized animals with oestradiol restored tumour weights to intact control levels. Oestradiol substitution of intact animals did not further enhance tumour growth. The growth of the primary tumour was inhibited by medroxyprogesterone acetate (MPA) at a dose of 100 mg/kg by 67% and by tamoxifen at a dose of 20 mg/kg by 38%. Lung metastases were regularly seen in both species, although to a lesser extent in nude mice than in DA/Han rats. Tamoxifen treatment did not alter the number of lung metastases, whereas MPA or ovariectomy produced a significant reduction in the number of lung metastases. The EnDA endometrial carcinoma of the DA/Han rat with respect to its oestrogen sensitivity, oestrogen receptor expression, morphology and metastatic growth, grossly resembles a typical endometrial adenocarcinoma and can therefore be regarded as auseful in vivo experimental model for the evaluation of new endocrine treatment strategies.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01215924
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  • 7
    Electronic Resource
    Electronic Resource
    Enhancement of the antitumor efficacy of the antiprogestin, onapristone, by combination with the antiestrogen, ICI 164384 (1994)
    Springer
    Journal of cancer research and clinical oncology 120 (1994), S. 298-302 
    Details
    ISSN: 1432-1335
    Keywords: Antiprogestin ; antiestrogen ; endocrine combination therapy ; experimental mammary tumor
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract So far, no combination of endocrine treatments has been routinely used in the therapy of breast Cancer. It was, therefore, our interest to determine whether the combination of the antiprogestin, onapristone (ON), and the pure antiestrogen, ICI 164384 (ICI), might provide a more effective therapy than either monotherapy in experimental mammary tumors containing both estrogen and progesterone receptors. In the MXT-mammary tumor of the mouse, ON (5 mg/kg) administered for 3 weeks exerted an ovariectomy-like antitumor effect (56% inhibition), whereas ICI (30 mg/kg) was weakly effective (28% inhibition). The combination of ON and ICI was, however, distinctly more effective than the monotherapies or ovariectomy, causing 78% inhibition. A similar potentation of antitumor effect by the combination was manifested in the dimethylbenzanthracene-induced mammary tumor of the rat when ON (5 mg/kg) and ICI (30 mg/kg) were administered once daily for 4 weeks (s.c.). The remission rates of tumors found after treatment with ICI, ON, the combination and ovariectomy (complete and partial remission) were 15%, 46%, 71% and 100% respectively. In the animals bearing DMBA-induced tumors, treatment with ON alone significantly increased the serum levels of luteinizing hormone and prolactin, but caused only a slight increase in the peripheral levels of estradiol and progesterone. ON had no appreciable effect on the uterine and ovarian weights. ICI reduced the uterine weight and the serum progesterone level. In the combination with ON, ICI reversed the effect of ON on the progesterone level without influencing the luteinizing harmone and prolactin levels. These findings suggest that the augmentation of antitumor effectiveness by the combination of two antihormones can be ascribed not only to their effects at estrogen- and progester-one-receptor-binding sites, but also to the decrease in the peripheral level of progesterone. Thus, an appropriate combination of antiprogestin and pure antiestrogen may be useful in the management of breast cancer.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01236387
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  • 8
    Electronic Resource
    Electronic Resource
    The tumour-inhibiting potential of the progesterone antagonist Onapristone in the human mammary carcinoma T61 in nude mice (1992)
    Springer
    Journal of cancer research and clinical oncology 118 (1992), S. 187-189 
    Details
    ISSN: 1432-1335
    Keywords: Onapristone ; Progesterone antagonist ; T61 mammary carcinoma ; Progesterone receptor
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The progesterone antagonist Onapristone proved to possess strong tumour-inhibiting activity in a panel of experimental mammary carcinomas. Its underlying mechanism of action is due to a progesterone-receptor-mediated induction of terminal differentiation and a specific blockade of the cell cycle and is also present in the absence of progesterone as was shown in the MXT mammary tumour. To prove this further, the tumour-inhibiting activity of Onapristone was investigated in the human postmenopausal T61 mammary tumour implanted in castrated male nude mice. Whereas Onapristone given alone had no effect on growth of established tumours, after stimulation of the relatively low progesterone receptor content of this tumour line with an oestrogen, Onapristone significantly inhibited tumour growth. Thus, we suggest that Onapristone exerts its antitumour action via progesterone receptors. As there is no endogenous progesterone in these mice, the tumour-inhibiting activity of Onapristone is not primarily due to a classical antihormonal effect.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01410132
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  • 9
    Electronic Resource
    Electronic Resource
    The tumor-inhibiting effect of diethylstilbestrol and its diphosphate on the Nb-H and Nb-R prostatic carcinomas of the rat (1990)
    Springer
    Journal of cancer research and clinical oncology 116 (1990), S. 159-167 
    Details
    ISSN: 1432-1335
    Keywords: Diethylstilbestrol ; Honvan ; Accessory sex organs ; Noble Nb prostate tumors ; Morphometry
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary For many years, diethylstilbestrol (DES) and its diphosphate (DESPP; Honvan) have been standard therapies for prostatic carcinoma. The effects of DES, its monophosphate (DESP) and of DESPP on the weights of accessory sex organs of mice and rats, and on the experimental Noble Nb-H and Nb-R prostatic carcinomas of the rat were, therefore, compared. In intact mature mice, all three compounds led to a strong and dose-dependent inhibition of seminal vesicle weights and testosterone levels, whereas only a slight antiandrogenic activity in castrated mice was found. In intact rats, DES, DESP and DESPP strongly inhibited accessory sex organ weights and testosterone levels. In castrated rats, however, no antiandrogenic activity was determinable. The prostate carcinoma-inhibiting effects of DES and DESPP were tested in comparison with castration in the transplantable hormone-sensitive Nb-H and Nb-R prostatic carcinoma in rats. Whereas castration caused only a retardation of tumor growth, DES and DESPP (3×0.1 mg/kg and 1.0 mg/kg weekly s.c.) led to an almost complete inhibition, which was significantly (P〈0.01) better than the effect of castration. As the weights of accessory sex organs were identically reduced by either castration or the estrogens, a direct tumor-inhibiting effect of DES and DESPP in addition to their testosterone-lowering activity is obvious. This was proved in an experiment with castrated rats. The only slightly inhibitory activity of castration was strongly potentiated by concomitant administration of DES. Moreover, histological examinations revealed that Nb-H and Nb-R tumors were much more damaged by treatment with DES or DESPP than after castration. Morphometry of the tumors showed that tumor reduction is associated with a decrease in the ratio of the epithelial to the stromal density, i.e. there was an even more pronounced decrease in epithelial cells than that found by merely measuring tumor area. These studies show that the prostate carcinoma-inhibiting effect of DES and DESPP in the Nb model is superior to the effect of castration and that they act directly on the tumor cells used, even in castrated rats.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01612671
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  • 10
    Electronic Resource
    Electronic Resource
    [meso-1,2-Bis(2,6-dichloro-4-hydroxyphenyl)ethylenediamine]-dichloroplatinum(II), a new drug not only parenterally but also orally active in the therapy of breast and prostate cancer (1993)
    Springer
    Journal of cancer research and clinical oncology 119 (1993), S. 707-716 
    Details
    ISSN: 1432-1335
    Keywords: Platinum complex ; Peroral administration ; Estrogenic activity ; Antitumor activity ; MXT(M3.2) mouse mammary tumor ; Noble Nb-R rat prostatic tumor ; Toxicity
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The platinum complex [meso-1,2-bis(2,6-dichloro-4-hydroxyphenyl)-ethylenediamine]dichloroplatinum(II), K, was tested for its antitumor activity on hormonesensitive tumor models under peroral administration. The resorption from the gastrointestinal tract was proved by determining the estrogenic effect of K in a dose/activity study using the immature-mouse uterine weight test. In comparison to the subcutaneous injection, a tenfold peroral dose was administered to achieve identical effects. By peroral treatment of the hormone-sensitive MXT(M3.2) mammary carcinoma of the mouse with K an almost complete inhibition of the tumor growth was obtained. This effect was superior to that of subcutaneously applied cisplatin and significantly better than that obtained by perorally administered ligand L at an equimolar dose, indicating that the antitumor effect is caused by the intact complex K and not by the liberated ligand L. The strong antitumor activity of perorally applied K was also demonstrated on the hormone-sensitive Noble Nb-R prostatic carcinoma of the rat. Histological examinations showed that the platinum complex K did not cause cisplatin-like kidney damage or irritations of gastric or intestinal mucosa when given perorally.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01195341
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