Anti-tumor activity

In this paper, the synthesis of arylidene heterobicyclicpyrimidinones and thiones is reported by condensation of aromatic aldehydes, cyclopentanone, and urea or thiourea in the present of FePO4 as the green and recyclable catalyst.

6p tocectocec 25-05-2020 24 1   Download

The benzoacronycine derivative, S23906-1, was character-ized recently as a novel potent antitumor agent through alkylation of theN2 positionof guanines inDNA.We show here that its reactivity towards DNA can be modulated by glutathione (GSH). The formation of covalent adducts between GSH and S23906-1 was evidenced by EI-MS, and the use of different GSH derivatives, amino acids and dipeptides revealed that the cysteine thiol group is absolutely required for complex formation because glutathione disul-fide (GSSG) and other S-blocked derivatives failed to react covalently with S23906-1. ...

12p fptmusic 16-04-2013 43 4   Download

The dimeric structure of seminal ribonuclease (BS-RNase) is maintained by noncovalent interactions and by two intersubunit disulfide bridges.Another unusual feature of this enzyme is its antitumour action, consisting in a cyto-toxic activity selective for malignant cells.This cytotoxic action is exerted when the protein reaches the cytosol of the affected cells, where it degrades ribosomal RNA, thus blocking protein synthesis and leading cells to death.

8p fptmusic 16-04-2013 43 2   Download

Onconase, a member of the ribonuclease superfamily, is a potent cytotoxicagent that isundergoingphase II/IIIhuman clinical trials as an antitumor drug. Native onconase from Rana pipiensand its amphibian homologs have an N-ter-minal pyroglutamyl residue that is essential for obtaining fully active enzymes with their full potential as cytotoxins. When expressed cytosolically in bacteria, Onconase is isolated with an additional methionyl (Met1) residue and glutaminyl insteadof a pyroglutamyl residue at position 1 of the N-terminus and is consequently inactivated....

9p dell39 03-04-2013 34 4   Download

The cytotoxic action of some ribonucleases homologous to bovine pancre-atic RNase A, the superfamily prototype, has interested and intrigued investigators. Their ribonucleolytic activity is essential for their cytotoxic action, and their target RNA is in the cytosol. It has been proposed that the cytosolic RNase inhibitor (cRI) plays a major role in determining the ability of an RNase to be cytotoxic.

11p inspiron33 25-03-2013 40 6   Download

Curcumin, a component of turmeric, has potent antitumor activity against several tumor types. However, its molecular target and mechanism of anti-proliferative activity are not clear. Here, we identified curcumin as a novel antimicrotubule agent. We have examined the effects of curcumin on cellu-lar microtubules and on reconstituted microtubules in vitro.

13p inspiron33 23-03-2013 52 4   Download

Ammonium trichloro(dioxoethylene-o,o¢)tellurate (AS101) is an organotel-lurium compound with pleiotropic functions that has been associated with antitumoral, immunomodulatory and antineurodegenerative activities. Tel-lurium compounds with a +4 oxidation state, such as AS101, react uniquely with thiols, forming disulfide molecules.

12p galaxyss3 19-03-2013 36 3   Download

Pladienolide is a naturally occurring macrolide that binds to the SF3b com-plex to inhibit mRNA splicing. It has not been fully validated whether the splicing impairment is a relevant mechanism for the potent antitumor activ-ity of pladienolide.

11p cosis54 08-12-2012 30 4   Download

Tuyển tập báo cáo các nghiên cứu khoa học quốc tế ngành y học dành cho các bạn tham khảo đề tài: Antitumor activity of mixed heat shock protein/ peptide vaccine and cyclophosphamide plus interleukin-12 in mice sarcoma

9p toshiba22 21-11-2011 56 6   Download