Antitumor bioactivity

An antitumor bioactivity glycoprotein is also purified from earthworm (E. fetida) recently [82], It is assayed by using a liver tumor model (H22) of mice the results show that significant antitumor effects and the life-prolonged rate was 65.4% in cultured H22 of mice [82]. Furthermore, it has been proved that EFE can enhance the curative effects by both radiation therapy and chemotherapy [83,84],... 

Rosazza JP (1978) Antitumor antibiotic bioactivation, biotransformation and deriva-tization by microbial systems. Recent Results Cancer Res 63 58-68... 

Gutierrez, P. L. The role of NAD(P)H oxidoreductase (DT-diaphorase) in the bioactivation of quinone-containing antitumor agents a review. Free Radio. Biol. Med. 2000, 29, 263-275. 

Bioactive C-glycosyl compounds are known since long time, C-nucleo-sides in particular, such as pirazomycin or showdomycin (Fig. 4), isolated from natural sources, showed a variety of interesting biological properties such as antitumor, antiviral or antibacterial activities.4... 

Fig. 8.17. Mechanism of bioactivation of self-immolative carbamate prodrugs of cytotoxic amines. A bacterial nitroreductase coupled to a tumor-directed antibody reduces the prodrug to a hydroxylamine (Reaction a), which breaks down spontaneously to liberate the antitumor...

Stoka, V., Turk, B., Schendd, S.L., Kim, T.-H., Cirman, T, Srripas, SJ., EUerby, L.M., Bredesen, L., Freeze, H, Abrahamson, M., Bromme, D., Krajewski, S., Reed, J.C., Yin, X.-M., Turk, V., and Salvesen G.S., 2001, Lysosomal Protease Pathways to Apoptosis. Cleavage of Bid, not pro-caspases, is the most likely route. J. Biol. Chem. 276 3149-3157 Srm, X. and Ross, D., 1996, Quinone-induced apoptosis in human colon adenocarcinoma ceUs via DT-diaphorase mediated bioactivation. Chem. Biol. Interact. 100 267-76 Taatjes, D.J. and Koch, T.H., 2001, Nuclear targeting and retention of anthracycUne antitumor dmgs in sensitive and resistant tumor ceUs. Curr. Med Chem. 8 15-29 Tarr, M. and van Helden, PT)., 1990, Inhibition of transcription by adriamycin is a... 

Sugar-derived a,(3-unsaturated lactones are relevant motifs considering their ability to act as functionalized substrates for a variety of transformations. Some of them are bioactive [218-222]. An early synthesis of the enantiomer of (+)-altholactone, a natural product with cytotoxic and antitumor activities (for a review on the bioactivity of styryUactones see [223, 224]), involves the preparation of a furanose-fused a,p-unsaturated 8-lactone intermediate 189 [225]. Starting from a a-D-xy/o-pentodialdofuranose derivative 187, aReformatsky reaction with ethyl bromoacetate introduces the carboxyhc side chain necessary for intramolecular lactonization (Scheme 46). 

Recently, marine fish-derived bioactive peptides have been shown to possess many physiological functions including antihypertensive, antioxidant, antimicrobial, antiproliferative, antitumor, anticoagulant, and immunomodulatory activities. Among these, antihypertensive peptides act as ACE inhibitors are of particular interest for prevention and treatment of hypertension (Kobayashi et ah, 2008). 

This chapter will focus on various classes of compounds that possess potent antitumor, anti-HIV, and antifungal activity recently discovered in my laboratory. These compounds were obtained by bioactivity- and mechanism of action-directed isolation and characterization... 

More recently, two new isonakafiiran-type sesquiterpenes were isolated from this sponge species [74], These types of compounds possess interesting antitumor and antifungal activity, and attempts to synthesize them are being conducted [75], Other bioactive metabolites, such as antifouling sesquiterpenes, have also been recently isolated from Dysidea herbacea [76],... 

In the course of our study on the rational design, synthesis and SAR of new antitumor taxoids, we became interested in incorporating fluorine(s) into paclitaxel and taxoids in order to investigate the effects of fluorine on cytotoxicity, blocking of known metabolic pathways, and its use as a probe for identifying bioactive conformation(s) of taxane antitumor agents. 

In the second section of the volume, N-hclerocycles such as phenothiazines, phenoxazines, dihydropyridines, and related compounds are shown also to have interesting biological activity including antitumor activity, vermicide, antibacterial activity, and antischizophrenic activity (i.e. chlorpromazine of the phenothiazine family and its analogs). The activity of phenothiazine and compounds such as phenoxazines and related heterocycles, and also recent bioactive mesoionic heterocycles will be discussed. 

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