Kooperativer Bibliotheksverbund

Berlin Brandenburg


Your email was sent successfully. Check your inbox.

An error occurred while sending the email. Please try again.

Proceed reservation?

  • 1
    Language: English
    In: Letters in Drug Design & Discovery, 2012, Vol.9(9), p.815-822
    Description: The anticancer drug candidate (1-methyl-3-(p-cyanobenzyl)benzimidazole-2-ylidene)silver(I)acetate (SBC1) was tested in vitro against human neuroblastoma cells, UKF-NB-3 and UKF-NB-6, delivering IC50 values of 29 +/- 5 and 29 +/- 4 μM, while further testing against cisplatin-, carboplatin- and oxaliplatin-resistant UKF-NB-3/6 sub-lines showed no cross-resistance with respect to SBC1. A similar trend was found for SBC1 against the human colon carcinoma cell line HCT8 with an IC50 value of 3.1 +/- 0.9 μM; SBC1 was again able to break cisplatin- and carboplatin-resistance in the corresponding sub-lines. SBC1 was also tested against the prostate cancer cell line PC-3 and its paclitaxel-resistant sub-line, which gave IC50 values of 14.1 +/- 0.9 and 14.5 +/- 0.8 μM, which indicated no cross-resistance with paclitaxel. In order to test the possible transport of SBC1 via albumin the binding of SBC1 against this transport protein was measured using a fluorescence titration, which gave an ΔG value of 28 +/- 3 kJ/mol. In circular dichroism and DNA denaturation assays SBC1 proved to be a strongly DNA-binding drug candidate. SBC1 was then given at 25 and 50 mg/kg/d, in four injections to two cohorts of eight CAKI-1 tumor-bearing NMRI:nu/nu mice, while a further cohort was treated with solvent only. At these two dosages SBC1 showed a borderline toxicity leading to mortality and body weight loss, while no significant tumor growth reduction or influence on blood parameter with respect to the solvent-treated control group was observed. Further in vivo testing against zebrafish larvae revealed significant toxicity of SBC1 at micromolar concentrations; no useable anti-angiogenic dosage was observed.
    Keywords: Anticancer Drug ; Anti-Angiogenic Drug ; Carbene-Silver Complex ; Renal Cell Cancer ; Albumin-Binding Assay ; Dnabinding Assay ; Xenograft Mouse Model ; Zebrafish Intersegmental Vessel Assay
    ISSN: 1570-1808
    E-ISSN: 1875-628X
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
  • 2
    Language: English
    In: Current medicinal chemistry, August 2002, Vol.9(15), pp.1417-33
    Description: The branched-chain fatty acid valproic acid (VPA) is the most commonly used antiepileptic drug for treating generalized epilepsy. Although originally considered to be of low toxicity, VPA has proved to possess considerable teratogenic potential when applied to the pregnant epileptic women. During the last few years, it has become evident that some of the mechanisms which account for the malformations produced by VPA are related to distinct anti-tumor properties of this compound. This intriguing discovery opens novel aspects for the treatment of tumor patients. In the present review, the biological, biochemical and pharmacological properties of VPA are discussed. Analyses of structure-activity relationships can provide the necessary insight into the molecular structures responsible for the anti-tumor effects.
    Keywords: Antineoplastic Agents -- Pharmacology ; Valproic Acid -- Analogs & Derivatives
    ISSN: 0929-8673
    E-ISSN: 1875533X
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
Close ⊗
This website uses cookies and the analysis tool Matomo. Further information can be found on the KOBV privacy pages