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 16 0   Download

Gossypol, a yellow pigment, isolated from cotton seeds, exhibits many interesting biological activities: antitumor, antimalarial, anti-HIV [1]. But gossypol is toxic and this toxicity may be related to the two-functional aldehyde groups [2]. Many authors prepared the Schiff’s’ base adducts of gossypol from 1985 to 2002, but these authors did not pay attention to the factor that these adducts may present under or the imine form or the enamine one.

5p uocvong04 24-09-2015 36 4   Download

Derivaties of 1,2,4-triazole and 1,3,4-oxadiazole have a lot of biological activities such as antifungi, antibiotic, antivirus, antitumor, etc. Nineteen hetero-compounds have been synthesized. Their structures have been confirmed by elemental analysis and the spectra methods as UV, IR and NMR. In this study, we focus on the analysis the first defragments on the mass-spectra of some compounds which is derivaties of 1,3,4-oxadiazole and 1,2,4-triazole.

5p uocvong04 24-09-2015 38 3   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 41 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 37 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 33 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 38 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 34 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 26 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 53 6   Download

Solid Tumors Small-molecule epidermal growth factor (EGF) antagonists act at the ATP binding site of the EGF receptor tyrosine kinase. In early clinical trials, gefitinib showed evidence of responses in a small fraction of patients with non-small cell lung cancer. Side effects were generally acceptable, consisting mostly of rash and diarrhea. Gefitinib was found to have antitumor activity mainly in the subset of patients with tumors containing activating mutations in the EGF receptor.

5p konheokonmummim 03-12-2010 79 4   Download

Cisplatin was discovered fortuitously by observing that bacteria present in electrolysis solutions could not divide. Only the cis diamine configuration is active as an antitumor agent. It is hypothesized that in the intracellular environment, a chloride is lost from each position, being replaced by a water molecule. The resulting positively charged species is an efficient bifunctional interactor with DNA, forming Pt-based cross-links.

5p konheokonmummim 03-12-2010 56 3   Download

The bevacizumab experience suggests that inhibition of the VEGF pathway will be most efficacious when combined with agents that directly target tumor cells. This also appears to be the case in the development of small-molecule inhibitors (SMI) that target VEGF receptor tyrosine kinase activity but are also inhibitory to other kinases that are expressed by tumor cells and important for their proliferation and survival.

6p konheokonmummim 03-12-2010 83 5   Download