Cytotoxicity activities against human tumor cell line

A similar trimerization strategy of acrolein (285) was used recently by Hong et al. (Scheme 76) early in the total synthesis of montiporyne F (334) (S02), a natural product isolated from the coral Montipora sp. exhibiting cytotoxic activity against human tumor cell lines (307). Importantly, trimerization of 285 in the presence of (5)-12 and several additives always provided the racemic dialdehyde 335. Although this is an example of a procedure where no stereodifferentiation... 

Isolated polypeptides, viscotoxins II, III, and IVb, have been associated with cardio-toxicity but have also been found to exhibit cytotoxic activity against human tumor cells of the KB and HeLa lines in tissue culture. A peptide with a molecular weight of 5000 was found to be cytotoxic to Dalton s lymphoma ascites tumor cells in vitro in mice, without affecting normal lymphocjfies, indicating a cell-dependent specificity also cyctotoxic to Ehrlich ascites cells, both prophylacticaUy and after tumor development. Commercial mistletoe products have been used to treat various cancers in Europe with clinical success. A group of 50 cases of carcinomatous pleural effusions were treated with a topical preparation for an average of 3.3 application over 18 days exudation disappeared in 92% of the patients. In postoperative ovarian cancer patients, a mistletoe preparation statistically increased survival. ... 

Rhenium tricarbonyl complexes containing substituted cyclopentadi-enyl and bis diphenylphosphine ligands also were investigated as anticancer agents. The antiproliferative effects on breast cancer of complex A shown in Fig. 23 were examined relative to the known active metabolite, 4-hydroxy tamoxifen, and found to have a similar effect [107]. The cytotoxicity of five rhenium tricarbonyl bis-diphenylphosphine complexes B shown in Fig. 23 was examined for 18 different human cancer cell lines. The tests showed that all the complexes were active against specific tumor cell lines, especially a line of breast and uterine cancer [108]. 

Very recently a family of diphenyltin(IV) compounds was tested in vitro against human tumor cell lines to assess their cytotoxic activity, and the same family of compounds was also tested for antioxidant efficiency in rat brain homogenate, showing that there is a structure-activity relationship in the latter case. The correlation suggests that selected molecular variables are prototype tracers for the calculation of inhibitory concentrations. Moreover there seems to be an inverse structure-response behavior among activities, since the most hydrophobic organotin molecule is the least active compound for cytotoxic assays, while it is the best in anti-oxidant tests. 

In the course of a search for antitumor compounds in dinoflagellates, the culture broths of two strains of Pr cf reticulatum showed extremely potent cytotoxicity against human tumor cell lines. The four equally active compounds, named protoceratins III, III, and TV, were purified and their structures were studied. The major compound (protoceratin I) was proved to be identical to homoYTX... 

Stable during isolation procedure in spite of nonprotein chromophore [310]. Later, an enantioselective synthesis of antibiotic N1999A2 also established the stereochemistry of 303 [311], The antibiotic exhibited remarkably potent antitumor activity against various tumor cell lines for instance, its IC50 of cytotoxicity to human colon carcinoma HCTllbcell was 6.0xl0 M [310],... 

In vitro cytotoxic activity was found against human leukemia (HL-60) cells exposed to coumarins (especially dipetaUne) and lignans (asarinin and sesamin) isolated from the root bark and fresh stems of northern prickly ash. Cytotoxic effects on human tumor cell lines were also found from crude extracts of the berries and furanocoumarins isolated therefrom (psoralen, isoimperatoin, and xanthox-toxin). The bark of southern prickly ash has shown in vitro growth inhibition of a methi-cillin-resistant strain of Staphylococcus aureus. Activity was largely attributed to the alkaloid chelerythrine, which showed activity against various other methicillin-resistant strains of the bacteria. ... 

Gielen and Willem studied the in vitro cytotoxicity of diorganotin trimethoxy benzoates against 60 hiunan tumor cell Unes. In general, they found that the dibutyltin compounds were more active against human cancer cell lines than were die dietiiyltin derivatives. 

Some of the [Au(N,0)Cl2] derivatives, namely 58a, 59a and 59b, which have been tested for cytotoxic activity against various human tumor cell lines, have shown significant effects [144]. Compound 57 is a potential alternative to dimethylgold (III) P diketonates and can be used as a starting material for gold coatings by the CVD method [140]. Recent studies have shown that the long-term stability of these... 

Figure 29) was tested in several cell lines in a one-dose in vitro primary cytotoxicity assay, and passed the criteria for activity (20-29% growth percentages) next, it was scheduled for evaluation against the full panel of 60 human tumor cell lines at minimum of five concentrations at 10-fold dilution, showing very favorable cytotoxicity <2003EJM781>. 

In 2002, Munro et al. reported the isolation of coproverdine (271) from a New Zealand Ascidian. The name of this isolate was derived from the descriptor attached to the voucher specimen (green sheep-shit-like in appearance), hence coproverdine copro Greek dung, ovis Latin sheep, verde Latin green). This alkaloid was isolated from Nature in optically active form [a]p — 8.0 (c 0.36, EtOH). However, the absolute configuration was not assigned. Coproverdine showed cytotoxic activity against a variety of murine and human tumor cell lines (240). 

Twenty-five cryptophycins, e.g. cryptophycin 1 (162), have been isolated from a Nostoc sp. strain. They exhibit various degrees of cytotoxicity against three tumor cell lines, namely KB (human nasopharyngeal), LoVo (human colorectal adenocarcenoma), and SKOV3 (human ovarian carcinoma). Removal of the chlorine atom leads to a 10-fold reduction in cytotoxicity [124]. The antitumor activity of a number of cryptophycins from Nostoc sp. has been evaluated [125]. 

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