Cytotoxic activities

Studies on the kinetics of formation of S2F2Q and reviews of appHcable Hterature have been reported (124—126). Other work has concentrated on the use of cell culture evaluation methods for assessing cytotoxic activity of SF decomposition products (127,128). Several laboratories seek to provide methods for accurately determining S2F2Q in operating electrical units (57). 

I IS. Hibbs-. B, Taintor, R. R., Vavrm, Z., and Rachlin, E. M. (1988). Nitric oxide A cytotoxic activated macrophage effector molecule. Biochem. Biophys. Res. Commun. 1.57, 87-99,... 

The adventitious discovery of the antitumor action of the nitrogen mustard poison war gases led to intensive investigation of the mode of action of these compounds. In brief, it has been fairly well established that these agents owe their effect to the presence of the highly reactive bis(2-chloroethyl)amine group. The cytotoxic activity of... 

Dysidazirine 130 was isolated by Ireland in 1988 from a Fijian sample of the marine sponge Dysidea fragilis [194] as the major lipophilic component of the sponge and was shown to possess cytotoxic activity against L1210 cells, as well as... 

British investigators (Haddow and Timmis 1951) synthesized and studied esters of the methanesulfonic acid. The most active derivative was the dimethylsulfonic ester of 1,4-butanedione, known as busulfan. Busulfan interacts with the thiol groups of proteins and amino acids some of its metabolites can alkylate the thiols of cysteine, peptides and proteins. Busulfan exerts selective cytotoxic activity in hematopoietic bone marrow cells and inhibits the formation of granulocytes and platelets. It slightly affects the lymphoid tissue. 

Human tumor necrosis factor (TNF) (Fig. 1) is a hormone-like proinflammatory peptide belonging to the group of cytokines. It is mainly produced by cells of the immune system in response to infection, inflammation, or cell damage. Disregulated TNF is an important factor in many pathological situations, like sqDsis, rheumatoid arthritis, inflammatory bowel disease (Crohn s disease), and Cachexia. The cytotoxic activity of TNF is of interest in development of new antitumoral strategies. 

TNF was originally identified because of its cytotoxic activity against some tumor cell lines and its ability to induce hemorrhagic necrosis of solid tumors in various animal models. However, the clinical use of TNF as an anticancer drug has been so far limited by its severe cardiovascular side effects. Therefore, TNF treatment is limited to regional and local administration of high doses of TNF, often in combination with chemotherapy, as accomplished in isolated limb and isolated hepatic perfusion (ILP and IHP, respectively) [5]. In the case of ILP, typically metastases are treated, patients benefit from this procedure by salvage of limbs from a loss by amputation. 

In contrast to this view, but in analogy with the behavior of several antitumor metal complexes, some authors proposed that the DNA is the probable target for cytotoxic activity of organotin(IV) compounds. In this section we survey and compare the most important literature data published to date on this subject. 

Seinen W, Penninks AH (1979) Immune suppression as a consequence of a selective cytotoxic activity of certain organometallic compounds on thymus and thymus-dependent... 

This indicates that endosulfan is capable of inducing chromosome breakage and loss. Endosulfan also induced cytotoxic activity (significant increase in the number of crossover colonies) in the yeast strain S. cerevisiae T2 (deficient in repair system), but not in S. cerevisiae T1 (L Vova 1984). 

The cytotoxic activities of the 2, 2 -difluoro analog (775) of 737 against Chinese hamster ovary and tumor cells, in comparison with those of 1- -d-arabinofuranosylcytosine ara-C, a drug for leukemia), have been studied 775 is transported the faster through membrane into cells, more effectively phosphorylated by the deoxycytidine kinase (to the 5 -mono-phosphate) and, after conversion into the 5 -triphosphate, more highly accumulated in the cells, with longer duration time, than is ara-C, but nevertheless 775 is incorporated into the DNA to a lesser extent than is ara-C. These characteristics of 775 were discussed. 

There is also evidence that individual chlorophyll derivatives exhibit cytostatic and cytotoxic activities against tumor cells. Studies have been started on electronic structures, in particular the electronic state of the phorphyrin macrocycle, and progress in this area is expected regarding photodynamic therapy for tumors, since the strong absorption of hght in the visible region is effective for laser excitation. Nevertheless, httle is known to date about the influences of peripheral groups on the electronic state of the macrocycle n system in chlorophyll derivatives. ... 

Pereira, E.M. et al., Tabebuia avellanedae naphthoquinones activity against methi-cillin-resistant staphylococcal strains, cytotoxic activity and in vivo dermal irritability analysis, Ann. Clin. Microbiol. Antimicrob., 22, 5, 2006. 

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... 

In 1985, it was reported by Hsiang et al. [43] that the cytotoxic activity of 20-(S)-camptothecin (CPT III) was attributed to a novel mechanism of action involving the nuclear enzyme topo I, and this discovery of unique mechanism of action revived the interest in CPT and its analogues as anticancer agents. CPT stabilizes the covalent, reversible topo I-DNA complex leading to the inhibition of DNA synthesis in mammalian cells and interferes with the topo I breakage-reunion reaction [44]. Clinical trials and structure-activity relationships have demonstrated the requirement of the a-hydroxy group, the... 

Font M et al. (2006) Structural characteristics of novel symmetrical diaryl derivatives with nitrogenated functions. Requirements for cytotoxic activity. Bioorg Med Chem 14(6) 1942-1948... 

Haliclonacyclamine F (25), arenosclerin D (26), and arenosclerin E (27) have been recently isolated from the sponge Pachychalina alcaloidifera endemic in Brazil [26]. The alkaloids 25-27 were isolated from the cytotoxic, antibiotic, and antituberculosis MeOH crude extract of P. alcaloidifera by a series of separations on silica-gel and cyanopropyl-bonded silica-gel columns. The structures of compounds 25-27 were established by the same approach employed for the structural elucidation of haliclonacyclamine E (13) and arenosclerins A-C (14-16) [18], as well as by comparison with NMR data for this last series of alkaloids. The alkaloids 25-27 displayed moderate cytotoxic activity against SF295 (human CNS), MDA-MB435 (human breast), HCT8 (colon), and HL60 (leukemia) cancer cell lines. 

Fx 39 Cytotoxic activity compound 39 showed good in vivo antitiunoral profile [38,223]... 

Indole alkaloids Strychnos icaja roots SiOj Hx + CHCI3 + MeOH + HjO AcOEt + iPrOH + NH3 aqueous DragendorlTs reagent UV Antimalarial, cytotoxic activity 14... 

Guerrero, I. C. Andres, L. S. Leon, L. G. Machin, R. P. Padron, J. M. Luis, J. G. Delgadillo, J. Abietane diterpenoids from Salvia pachyphylla and S. clevelandii with cytotoxic activity against human cancer cell lines. J. Nat. Prod. 2006, 69, 1803-1805. 

Labiatae) chemical diversity, phytogeographical significance, and cytotoxic activity. Chem. Divers. 2005, 2, 738-747. 

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