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  • 1
    Electronic Resource
    Electronic Resource
    Estramustine Phosphate Inhibits Microtubule Assembly by Binding to the Microtubule-Associated Proteins (1986)
    Oxford, UK : Blackwell Publishing Ltd
    Annals of the New York Academy of Sciences 466 (1986), S. 0 
    Details
    ISSN: 1749-6632
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Natural Sciences in General
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1111/j.1749-6632.1986.tb38413.x
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  • 2
    Electronic Resource
    Electronic Resource
    Cytotoxicity and metabolism of prednimustine, chlorambucil and prednisolone in a Chinese hamster cell line (1986)
    Springer
    Cancer chemotherapy and pharmacology 16 (1986), S. 85-90 
    Details
    ISSN: 1432-0843
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Prednimustine and chlorambucil induce dose-and time-dependent cell death in V79 Chinese hamster cells in vitro. Prednimustine was found to be 3–4 times more potent than either chlorambucil or an equimolar mixture of its components chlorambucil and prednisolone after 24 h treatment. Prednimustine was hydrolyzed to prednisolone and chlorambucil in the system, and the concentration of prednimustine was reduced by one half within 15 h. Prednisolone was not further metabolized, but chlorambucil was rapidly inactivated by dechlorination, the half-life being 2.5 h. No dechlorinated prednimustine was formed during the experiments. The higher stability of prednimustine than chlorambucil is probably due to protective binding to different serum proteins from those that bind chlorambucil. Substitution of fetal calf serum by human serum albumin revealed that hydrolysis of prednimustine is catalyzed by esterases present in the serum. In similar substitution experiments cell survival studies indicated that prednimustine itself was not cytotoxic. Rather, cytotoxicity was found to correlate with hydrolysis to chlorambucil. Thus, it appears that the prolonged availability of chlorambucil is responsible for the increased potency of prednimustine in this system.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00256154
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  • 3
    Electronic Resource
    Electronic Resource
    Comparison of estramustine with its dihydroxy analogue, estradiol 3-bis(2-hydroxyethyl)carbamate (1995)
    Springer
    Structural chemistry 6 (1995), S. 371-376 
    Details
    ISSN: 1572-9001
    Keywords: X-ray crystal structure determination ; antitumor agent ; nitrogen mustard
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Estramustine is an antimicrotubule agent that is effective against prostate cancer when used in combination with other microtubule-binding drugs. It is a derivative of estradiol and has a nitrogen mustard group attached via an intervening carbamate group. The molecular dimensions published for estramustine from crystal structure analyses (Mol. Pharmacol. 41∶569, 1992) indicate that the carbamate group modifies the mustard group by giving considerable double-bond character to the C-N bond. As a result the mustard group cannot form an active aziridine ring and therefore does not show the expected alkylating function. The substitution at O(3) of the aromatic A ring of the steroid moiety has also modified its activity as a steroid. Geometric data are presented here on a compound in which the two chlorine atoms of the mustard group of estramustine are replaced by hydroxyl groups. The question was, why does the dihydroxy derivative not show biological activity when chlorine atoms do not appear to be activated in estramustine itself? A comparison of the molecular geometries of the two compounds shows that the dimensions of the carbamate group are similar in both compounds. Therefore it appears that it is the extensive hydrogen-bonding capability of the dihydroxy compound that destroys its estramustine-like activity. In crystals of both compounds there is a hydrogen bond between O(17) -H and O(19) of another molecule, but the dihydroxy compound can form two more hydrogen bonds. This may possibly prevent it from reaching the site of action of estramustine or, if it does reach that site, cause it to behave differently.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF02310178
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  • 4
    Electronic Resource
    Electronic Resource
    Anti-tumour, toxicological and pharmacokinetic properties of a novel taurine-based nitrosourea (TCNU) (1988)
    Springer
    Investigational new drugs 6 (1988), S. 19-30 
    Details
    ISSN: 1573-0646
    Keywords: TCNU ; BCNU ; CCNU ; MeCCNU ; chlorozotocin
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary A novel nitrosourea, 1-(2-chloroethyl)-3-[2-(dimethylaminosulfonyl) ethyl]-1-nitrosourea (TCNU) tauromustine, has been investigated in a broad anti-tumour screen and, in depth toxicology and initial pharmacokinetics carried out. TCNU and its two metabolites were found to exhibit equal or better oral efficacy than that of BCNU, CCNU, MeCCNU or chorozotocin against L1210 leukemia, Walker mammary carcinoma, Lewis Lung, Harding Passey melanoma and colon carcinoma C26. The toxicological profile of TCNU after acute and 3 months treatment was similar in mice and rats to that of CCNU, with the exception that, TCNU did not cause the chronic liver disturbances found for CCNU. In dogs treated for 6 weeks with TCNU leucopenia and thrombocytopenia were the major side effects. Parent TCNU was found in all dogs. The absorption was fast, the maximum level being reach after 25 mins and the mean absorption time was 22 mins. The mean half life was 16.1 mins after intravenous and 17.4 after oral administration. The combination of these factors make TCNU an interesting clinical candidate.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00170775
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    Paper (German National Licenses)
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