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  • 1
    Electronic Resource
    Electronic Resource
    s.l. : American Chemical Society
    Inorganic chemistry 26 (1987), S. 844-846 
    ISSN: 1520-510X
    Source: ACS Legacy Archives
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1520-510X
    Source: ACS Legacy Archives
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
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  • 3
    ISSN: 1520-510X
    Source: ACS Legacy Archives
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
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  • 4
    ISSN: 1432-0843
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Two new platinum-containing phosphonate compounds,cis-diammine[nitrilotris(methylphosphonato)(2-)-O 1,N 1]platinum(II) (AMDP) andcis-cyclohexane-1,2-diamine[nitrilotris(methylphosphonato)(2-)-O 1,N 1]platinum(II) (DADP) were investigated in acetoxymethylmethylnitrosamine-induced autochthonous colorectal rat adenocarcinoma in vivo as well as in two human colon-cancer cell lines (SW707 and SW948) in vitro. In the in vivo model, the two compounds were given i.v. at doses of 8 and 13 mg/kg as well as p.o. at 16 and 26 mg/kg twice a week for 10 weeks, respectively. AMDP produced more intensive toxicity at both doses but showed higher antitumour activity only following i.v. administration. On the other hand. DADP caused significant tumour-growth inhibition after both modes of application, but as it produced only low toxicity, its use should be favoured. The in vitro assays were performed using two cell lines derived from human colorectal adenocarcinomas. According to the microculture tetrazolium test (MTT) AMDP (IC50, 34 and 59 μm in SW707 and SW948, respectively) was more effective than DADP (IC50, 412 and 660 μm in SW707 and SW948, respectively) in inhibiting cell growth. Based on cell counts AMDP (IC50, 8 and 11 μm in SW707 and SW948, respectively) and DADP (IC50, 266 and 285 μm in SW707 and SW948, respectively) showed more intensive antiproliferative efficacy as determined by the Coulter Counter method vs the MTT assay. The promising activities of these new platinum-linked phosphonic acids in autochthonous rat colorectal carcinoma and in human colorectal cancer cell lines warrant further investigations of compounds of this class to elucidate their role in the treatment of colorectal cancer.
    Type of Medium: Electronic Resource
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  • 5
    ISSN: 1432-0843
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The activity of the newly synthesized ruthenium derivative imidazolium-bis(imidazole)tetrachlororuthenate (III) [ImH(RuIm2Cl4)] was compared with that of 5′-deoxy-5-fluorouridine (5′dFUR) in autochthonous acetoxymethyl-methylnitrosamine (AMMN)-induced colorectal cancer in SD rats. Following coloscopic diagnosis of colorectal tumors treatment was administered twice weekly for a 10-week period. ImH(RuIm2Cl4) exhibited considerable antitumoral efficacy compared with 5′dFUR (20 T/C % and 60 T/C %, respectively) against the growth of AMMN-induced colorectal adenocarcinoma in SD rats. The mortality rates with ImH(RuIm2Cl4) were dose-related, but its efficacy did not vary in all doses administered.
    Type of Medium: Electronic Resource
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  • 6
    Electronic Resource
    Electronic Resource
    Springer
    Journal of cancer research and clinical oncology 116 (1990), S. 453-458 
    ISSN: 1432-1335
    Keywords: Cisplatin-containing phosphonic acids ; Osteosarcoma cell clones ; In vitro studies
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Osteosarcoma treatment still is unsatisfactory owing to the development of metastases. This situation causes many problems for the patients as well as the clinicians. Tumor heterogeneity is made responsible for the development of cell lines resistant to chemotherapy. As the transplantable osteosarcoma of the rat resembles the human metastasizing osteosarcoma, studies on clones of this tumor were started. The following compounds were investigated: AMDP,cis-diammine[nitrilotris(methylphosphonato)(2-)-O 1,N 1]platinum II; DADP,cis-cydohexane-1,2-diamine[nitrilotris(methylphosphonato)(2-)-O 1,N 1]-platinum II; IMD,cis-diammine[iminobis(methylphosphonato)(2-)-O 1,N 1]platinum II; DIMD,cis-cyclohexane-1,2-diamine[iminobis(methylphosphonato) (2-)-O 1,N 1]platinum II. In vitro assays were performed with cell lines derived from a lung metastasis with the limited-dilution method. The clones varied in modal chromosome number, growth kinetics and tumorigenicity. AMDP was the most potent compound in all three clones resulting in a concentration- and time-dependent effect while IMD was somewhat less active. The diamminocyclohexane derivatives were considerably less effective, inhibiting cell growth especially in clone C10. In contrast, clone C36 was more sensitive than C25 and did not recover within the observation period of 5 days. Viability was reduced significantly only in C10, when treated with AMDP. Differences between the clones and the various compounds in inhibiting cell growth could be observed. Therefore, further experiments on the heterogeneity and sensitivity of these cell lines seem promising.
    Type of Medium: Electronic Resource
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  • 7
    ISSN: 1432-1335
    Keywords: Bis-β-diketonato metal complexes of titanium, zirconium, and hafnium ; Budotitane ; Acetoxymethylmethylnitrosamine-induced autochthonous colorectal tumors ; Antitumor activity
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Bis-β-diketonato complexes of titanium, zirconium, and hafnium were tested against autochthonous colorectal tumors in rats. The model was found to reflect the clinical situation most closely. of the compounds tested, budotitane was the most effective in terms of decrease in tumor weight and number and in increasing the lifespan of the treated animals. The therapeutic efficiency was superior to that of 5-fluorouracil, which so far has been the drug with the best activity in patients suffering from colon cancer.
    Type of Medium: Electronic Resource
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  • 8
    ISSN: 1432-1335
    Keywords: Bisphosphonates ; Osteosarcoma ; Bone metastasis ; Prophylactic treatment ; Anticancer-agent-linked phosphonates
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Bisphosphonates are compounds with a high affinity for bone and other calcified tissues. They inhibit tumor-induced bone destruction and the associated hypercalcemia by hindering the activity of the osteoclasts. Owing to a long biological half-life of bisphosphonates in the bone, a treatment using a prophylactic regimen seems possible. This paper summarizes preclinical studies with the bisphosphonate 3-amino-1-hydroxypropylidene-1, 1-diphosphonic acid and two methyl derivatives; S-N,N-dimethylamino-1-hydroxypropylidene-1,1-diphosphonic acid and 4-N,N-dimetyhlamino-1-hydroxybutylidene-1, 1-diphosphonic acid with respect to their bone-protecting activity in therapy as well as in prophylaxis. To find substances that are useful for the treatment of primary tumor, as well as bone metastasis, we synthesized and testedcis-diammine[nitrilotris(methylphosphonato) (2-)-O 1 ,N1]platinum(II) andcis-diammine{[bis-(phosphonatomethyl)amino]acetato(2-)-O1, N1} platinum(II), which contain both an osteotropic and an antineoplastic moiety. Experiments were carried out: (a) in the intratibial transplanted Walker carcinosarcoma 256B of the rat, which mimics osteolytic bone metastasis, and (b) in the transplantable osteosarcoma of the rat, which shows a histology and metastatic pattern similar to that found in man. These investigations indicate that it is possible to effect adjuvant therapy of bone metastases by combination of two compounds with different properties into one structure without losing the therapeutic characteristics of the parent compounds. They thus provide evidence that it may be possible to design compounds well suited for the therapeutic or prophylactic treatment of bone-related malignancies.
    Type of Medium: Electronic Resource
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  • 9
    ISSN: 1432-1327
    Keywords: Key words Cisplatin ; Nucleoside monophosphates ; Capillary electrophoresis ; Platinum complexes ; Matrix-assisted laser-desorption ionization mass spectrometry
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract The binding behaviour as well as the time-dependent reaction of five platinum(II) complexes with 5′-GMP have been investigated by capillary electrophoresis under simulated physiological conditions referred to chloride concentration, pH and temperature. Different amine ligands influenced the binding properties towards 5′-GMP and resulted in different half-times of the overall reaction. Complexes with bidentate ligands reacted faster with the monophosphate compared to complexes with monodentate ligands. Complexes consisting of two monodentate hydroxyethylamine ligands reacted very slowly owing to a competitive intramolecular reaction of the hydroxyethyl residues, which was proven by NMR investigations. Reducing the number of hydroxyethyl residues increased the half-times of the reactions. Moreover, the major adducts formed with 5′-GMP were identified by MALDI-MS analysis.
    Type of Medium: Electronic Resource
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  • 10
    Electronic Resource
    Electronic Resource
    Springer
    Journal of cancer research and clinical oncology 111 (1986), S. 166-168 
    ISSN: 1432-1335
    Keywords: Ruthenium complex ; Imidazolium-bisimidazoletetrachlororuthenate (III) ; Antitumor activity ity
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The antitumor activity of imidazolium-bisimidazole-tetrachlororuthenate (III) against the P388 leukemia and against the B16 melanoma was investigated. The test compound showed high activity against these tumor models. The tumor inhibiting effect was in the range or better than the effects of the compounds cyclophosphamide, cisplatin, or 5-fluorouracil, which were tested as positive controls. The effective substance is a new, water soluble, anionic, nitrogen-heterocyclic coordinated, ruthenium species, exhibiting antitumor activity.
    Type of Medium: Electronic Resource
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