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  • 1
    Electronic Resource
    Electronic Resource
    Springer
    Journal of cancer research and clinical oncology 121 (1995), S. 193-202 
    ISSN: 1432-1335
    Keywords: Hyaluronidase ; Vinblastine ; Human melanoma models ; Nude mouse ; Combination therapy ; Enhancement of antitumor activity ; Long-term remission
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The regional chemotherapy of the human malignant melanomas (SK-MEL-2, -3, -5, -24) implanted in NMRInu/nu mice with a combination of the hyaluronic-acid-cleaving enzyme hyaluronidase (HYase) and vinblastine is a very effective therapeutic procedure. In three out of four melanoma models (SK-MEL-2,-3, -5) the weekly peritumoral administration of high-dose HYase (100 000 IU/kg) 4 h prior to the injection of 0.3 mg/kg vinblastine in the vicinity of the tumor (seven weekly therapeutic cycles) caused marked antitumor effects, while HYase and vinblastine were inactive when given alone. The pretreatment with HYase, which is well tolerated by the test animals, prevented local inflammation reactions commonly seen after subcutaneous vinblastine administration. Tumor growth and metastatic behavior of the melanomas used were neither increased nor reduced by HYase after peritumoral administration without subsequent vinblastine injection. The curative activity of the regional chemotherapy with HYase/vinblastine could be demonstrated on the SK-Mel-3 melanoma. After an observation time of 18 weeks tumor cells could no longer be detected in the subcutaneous region of the former lesion. Only macrophages, which had abundantly incorporated melanin, gave evidence of previously growing tumors. In contrast to the controls, no metastases could be observed in the axillary lymph nodes of the test animals.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1432-1335
    Keywords: miltefosine ; Cisplatin analogues ; MXT mouse mammary tumours ; Combination therapy
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Miltefosine, an alkylphosphocholine structurally related to alkyllysophospholipids showed highly selective antitumour activity against the hormone-sensitive variant of the s.c. transplantable MXT mouse mammary adenocarcinoma, the ovary-dependent MXT (M3.2), whereas it was inactive against the hormone-insensitive MXT (M3.2) OVEX variant. A dose of 32 mg/kg miltefosine p.o. daily for 5 weeks was well tolerated. Histopathological evaluation gave no signs of gastroenteral toxicity. After therapy the microarchitecture of the MXT (M3.2) tumours changed from that of a moderately differentiated adenocarcinoma to that of an anaplastic mammary carcinoma. A dose of 16 mg/kg miltefosine p.o. daily, though in effective per se, enhanced the antitumour activity of suboptimal i.p. doses of cisplatin and the hormone-like platinum analogue [meso-1,2-bis(2,6-dichloro-4-hydroxyphenyl)ethylenediamine]dichloroplatinum(II). Furthermore, it was shown, that miltefosine exhibited no (anti)hormonal properties. However, the mechanism of action of miltefosine remains unclear.
    Type of Medium: Electronic Resource
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  • 3
    ISSN: 0009-2940
    Keywords: Chemistry ; Inorganic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Antitumor Active cis-Platinum(II) Complexes with α-Amino Acid Esters and Peptide Esters. X-Ray Structure of cis-Dichlorobis(glycylglycine ethyl ester)platinum(II)A series of cis-platinum(II) complexes X2PtL2 (1-4) (X = halide, 2X = oxalate, malonate; L = α-amino acid ester, peptide ester) has been obtained from Pt42- and L. The dipeptide ester complexes are also accessible via peptide synthesis at the complex from Cl2Pt(NH2CHRCO2H)2 and α-amino acid esters using carbodiimide as coupling agent and the platinum atom as amino protecting group. The complexes Cl2PtL2 with α-amino acid ester ligands have also been prepared from the bis(chelate) compounds cis-Pt(NH2CHRCO2)2 and alcohol in the presence of HCl. The complexes have been characterized by their spectroscopic data, cis-Cl2Pt(GlyGlyOEt)2 (2a) by an X-ray analysis.
    Notes: Eine Reihe von cis-Platin(II)-Komplexen X2PtL2(1-4) (X = Halogenid, 2X = Oxalat, Malonat; L = α-Aminosäureester, Peptidester) wird aus PtX42- und L erhalten. Entsprechende Komplexe mit Dipeptidester-Liganden sind auch durch Peptidsynthese am Komplex aus Cl2Pt-(NH2CHRCO2H)2 und α-Aminosäureestern mit Carbodiimid als Kupplungskomponente und Platin als Aminoschutzgruppe zugänglich. Die Verbindungen Cl2PtL2 mit α-Aminosäureester-Liganden lassen sich auch aus den Bis(chelat)-Komplexen cis-Pt(NH2CHRCO2)2 und Alkohol in Gegenwart von HCl gewinnen. Die cis-Struktur der Verbindungen wurde spektroskopisch, die von Cl2Pt(GlyGlyOEt)2 (2a) durch Röntgenstrukturanalyse nachgewiesen.
    Additional Material: 2 Ill.
    Type of Medium: Electronic Resource
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  • 4
    Electronic Resource
    Electronic Resource
    Weinheim : Wiley-Blackwell
    Berichte der deutschen chemischen Gesellschaft 124 (1991), S. 2381-2389 
    ISSN: 0009-2940
    Keywords: Platinum complexes ; 1,2-Ethanediamines, 1,2-diaryl- ; Antitumor activity ; Chemistry ; Inorganic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: Various erythro- and threo-configurated dichloro[1-(hydroxyphenyl)-2-phenyl-1,2-ethanediamine]platinum(II) complexes were synthesized with the hydroxy group located in either the 2-, 3-, or 4-position of the phenyl ring (38-40). The diastereoisomeric 1-(3-hydroxyphenyl)-2-phenyl-1,2-ethanediamines (31, 32) and threo-1-(2-hydroxyphenyl)-2-phenyl-1,2-ethanediamine (30) were obtained by reduction of the 1,2-diazidoethanes and subsequent ether cleavage. The configuration of the threo-1,2-diazido-1-(2-methoxyphenyl)-2-phenylethane (5) was elucidated by X-ray analysis. The reduction of the erythro-1,2-diaryl-1,2-diazidoethanes, substituted with a methoxy group in ortho or para position, results in elimination reactions with formation of side products. The desired 1,2-diaryl-1,2-ethanediamines were finally synthesized via either an aziridine derivative 21 or by reduction of the respective dioximes 27, 28. The diamine ligands were converted into the corresponding dichloroplatinum(II) complexes 38 - 40.
    Additional Material: 3 Ill.
    Type of Medium: Electronic Resource
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  • 5
    Electronic Resource
    Electronic Resource
    Weinheim : Wiley-Blackwell
    Berichte der deutschen chemischen Gesellschaft 91 (1958), S. 862-864 
    ISSN: 0009-2940
    Keywords: Chemistry ; Inorganic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: Das Verteilungsverfahren nach L.C. Craig erlaubt auch die Auftrennung von Stereoisomerengemischen. Am Beispiel des N,N′-Dibutyl-α,α′-diphenyl-äthylendiamin-dihydrochlorids wird zunächst die Trennung in Meso- und Racemform gezeigt.
    Type of Medium: Electronic Resource
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  • 6
    Electronic Resource
    Electronic Resource
    Weinheim : Wiley-Blackwell
    Berichte der deutschen chemischen Gesellschaft 89 (1956), S. 1918-1921 
    ISSN: 0009-2940
    Keywords: Chemistry ; Inorganic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: Es wird über einen abweichenden Verlauf der Grignard-Reaktion bei Schiffschen Basen berichtet. Bei der Umsetzung hochverzweigter Alkymagnesiumhalogenide mit Benzylidenalkylaminen ergeben sich nicht die erwarteten Verbindungen vom Typ der l-Phenyl-l-alkylamino-alkane, sondern Diphenyläthylendiaminderivate.
    Type of Medium: Electronic Resource
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  • 7
    Electronic Resource
    Electronic Resource
    Weinheim : Wiley-Blackwell
    Liebigs Annalen 1980 (1980), S. 409-415 
    ISSN: 0170-2041
    Keywords: Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Thermolysis of ortho-Chloro-Substituted 1,2-DiarylethylenediaminesOn heating bis(2,6-dichlorophenyl)ethylenediamines 1a - d give indoles and  -  in the case of the racemates 1b and d  -  tetrahydroindoloindoles. The d,1-form of the corresponding 2,4-dichloro compound 1f leads to a 2,4,5-triarylimidazolidine, the meso-form 1e to an aziridine, whose formation via a 2,cis-4,5-triarylimidazolidine appears likely from mechanistic considerations.
    Notes: Die Bis(2,6-dichlorphenyl)ethylendiamine 1a - d reagieren bei der Thermolyse zu Indolen und im Falle der Racemate 1b und d auch zu Tetrahydroindoloindolen. Die d,1-Form der entsprechenden 2,4-Dichlorverbindung 1f führt zu einem 2,4,5-Triarylimidazolidin, die meso-Form 1e zu einem Aziridin, dessen Bildung über ein 2,cis-4,5-Triarylimidazolidin durch mechanistische Betrachtungen wahrscheinlich gemacht werden konnte.
    Additional Material: 1 Tab.
    Type of Medium: Electronic Resource
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