By a News Reporter-Staff News Editor at Clinical Trials Week -- Data detailed on Apoptosis have been presented. According to news reporting originating in Burgos, Spain, by NewsRx journalists, research stated, "In this Account, we discuss the development of new lipid bilayer anion transporters based on the structure of anionophoric natural products (the prodigiosins) and purely synthetic supramolecular systems. We have studied the interaction of these compounds with human cancer cell lines, and, in general, the most active anion transporter compounds possess the greatest anti-cancer properties."
The news reporters obtained a quote from the research from the University of Burgos, "Initially, we describe the anion transport properties of synthetic molecules that are based on the structure of the family of natural products known as the prodiginines. Obatoclax, for example, is a prodiginine derivative with an indole ring that is currently in clinical trials for use as an anti-cancer drug. The anion transport properties of the compounds were correlated with their toxicity toward small cell human lung cancer GLC4 cells. We studied related compounds with enamine moieties, tambjamines, that serve as active transporters. These molecules and others in this series could depolarize acidic compartments within GLC4 cells and trigger apoptosis. In a study of the variation of lipophilicity of a series of these compounds, we observed that, as log P increases, the anion transport efficiency reaches a peak and then decreases. In addition, we discuss the anion transport properties of series of synthetic supramolecular anion receptor species. We synthesized trisureas and thioureas based on the tren backbone, and found that the thiourea compounds effectively transport anions. Fluorination of the pendant phenyl groups in this series of compounds greatly enhances the transport properties. Similar to our earlier results, the most active anion transporters reduced the viability of human cancer cell lines by depolarizing acidic compartments in GLC4 cells and triggering apoptosis. In an attempt to produce simpler transporters that obey Lipinski's Rule of Five, we synthesized simpler systems containing a single urea or thiourea group. Once again the thiourea systems, and in particular a thiourea with a pendant indole group, transported anions efficiently. A series of related compounds containing a pendant trifluoromethyl group showed enhanced transport and significant anticancer properties. Researchers still need to determine of the exact mechanism of how these compounds depolarize acidic organelles within cancer cells."
According to the news reporters, the research concluded: "However, this work shows that these transporters based upon both natural products and purely synthetic supramolecular systems transport anions, depolarize acidic compartments within cancer cells and trigger apoptosis."
For more information on this research see: Anion Transporters and Biological Systems. Accounts of Chemical Research, 2013;46(12):2801-2813. Accounts of Chemical Research can be contacted at: Amer Chemical Soc, 1155 16TH St, NW, Washington, DC 20036, USA. (American Chemical Society - www.acs.org; Accounts of Chemical Research - www.pubs.acs.org/journal/achre4)
Our news correspondents report that additional information may be obtained by contacting P.A. Gale, Univ Burgos, Fac Ciencias, Dept. of Quim, Burgos 09001, Spain. Additional authors for this research include R. Perez-Tomas and R. Quesada (see also Apoptosis).
Keywords for this news article include: Spain, Burgos, Europe, Anions, Cancer, Oncology, Thiourea, Apoptosis, Nanotechnology, Supramolecular, Sulfur Compounds, Emerging Technologies, Clinical Trials and Studies
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