Cytotoxic value

Meegan et al. reported the synthesis of a number of [3-lactams and these were evaluated in a series of in vitro assays, which determined their antiproliferative activity in MCF-7 and MDA-MB-231 breast cancer cell lines and also their affinity for the oestrogen receptor (Fig. 6). The cytotoxicity of the [3-lactams was determined in the LDH assay to establish that the antiproliferative effects observed were due to cytostasis rather than cellular necrosis. Most of the compounds demons-treated low cytotoxicity, indicating that their action is cytostatic rather than cytotoxic. Cytotoxicity values considerably below that obtained for tamoxifen (13.4%, 10 pM) were observed with a most potent compound (3%, 10 pM in MCF-7 cell... 

The data are presented in different tables according to the main subclasses of flavonoids. Tables are divided in four columns that include the flavonoid subclass substituent, its trivial name, the type of tumor cell line inhibited and the reference. Cytotoxic values are not presented because the authors use different protocols and different times of incubation of flavonoids with cancer cells and the results would not be comparable. The order of each flavonoid in a Table is based firstly in the number of substituents, then in their position and finally in the type of substituent. Sometimes, the structure of a flavonoid does not appear in the tables, generally because it has a complicated structure. In such cases, you can find it in the reference or in the NCI database, using the NSC-number (http //dtp.nci.nih.gov/). 

Measure incorporated or 14C-protein hydrolysate in a b-scintillation counter. Plot the concentration against the 14C- uptake values and calculate the 50% cytotoxicity value (CC50) (Table 1). 

FK-506 (37) interferes with IL-2 synthesis and release and has a cyclosporin-like profile, but is considerably more potent in vitro. IC q values are approximately 100-fold lower. This neutral macroHde suppresses the mixed lymphocyte reaction T-ceU proliferation generation of cytotoxic T-ceUs production of T-ceU derived soluble mediators, such as IL-2, IL-3, and y-IFN and IL-2 receptor expression (83). StmcturaHy, FK-506 is similar to sirolimus. Mycophenolate mofetil (33), brequinar (34), and deoxyspergualin are in various phases of clinical evaluation. Identification of therapeutic efficacy and safety are important factors in the deterrnination of their utiUty as immunosuppressive agents. 

Sun et al. [41] synthesized a series of benzimidazoles (II) and evaluated their topo I-mediated cleavage as well as cytotoxicity against four cancer cell fines. Topo I cleavage values are reported as REC, the relative effective concentration (i.e., concentrations relative to that of Hoechst 33342, whose value... 

Zhu et al. [55] also synthesized a series of ester/amide derivatives of 2,3-dimethoxy-8,9-methylenedioxy-benzo[z]phenanthridine-12-carboxyhc acid (X) and evaluated their topo I-targeting activity as well as cytotoxicity against different cell lines. Topo I cleavage values are given as REC, the relative ef-... 

ICso is defined as the concentration of drug required to inhibit cell growth by 50% compared to a control. The IC50 values were calculated from the graphs obtained from the in vitro cytotoxicity assays and are the average of three independent experiments, each performed in triplicate. 

The combination of hydrophilic and hydrophobic parts of a molecule defines its amphiphilicity. A program has been described to calculate this property and calibrated against experimental values obtained from surface activity measurements [133]. These values can possibly be used to predict effect on membranes leading to cytotoxicity or phospholipidosis, but may also contain information, not yet unraveled, on permeability. Surface activity measurements have also been used to make eshmates of oral absorphon [126]. 

Table 1 Cytotoxicity towards A2780, A2780cisR, HT29 and A549 cancer cells, and ECRF24 endothelial cells, and intracellular uptake in A2780 cells and logP0/w values of 1 - 3. Errors represent the standard error of the mean (SEM)...

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