© WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
Editorial Board Chairs: Antonello Mai, Rainer Metternich. Assoc. Editors: David Peralta, Scott Williams (Sr)
Impact Factor: 2.98
ISI Journal Citation Reports © Ranking: 2015: 18/59 (Chemistry Medicinal); 77/255 (Pharmacology & Pharmacy)
Online ISSN: 1860-7187
August 30, 2010
ChemMedChem 09/2010: Fighting Cancer
Our September issue includes work by Opatz and colleagues, who report their short and versatile synthesis of emetine mimetics, helping to establish structure–activity relationships for this class of polycyclic alkaloids. Heme oxygenases (HO) are gradually being recognized as potential targets to address neurological, circulatory, and immune system problems, and so Szarek and co-workers report their research on azole-based compounds as HO inhibitors. The urotensin^^II peptide is an extremely potent vasoconstrictor; antagonists of its receptor (UT2R) are foreseen to have high therapeutic value. To get a better handle on antagonist selectivity between species isoforms of the UT2R, Goddard^^III and colleagues generated 3D model structures of rat and human UT2R, and comparison of the two, using known antagonists, revealed the basis for selectivity. In an effort to improve our understanding of the key interactions acetylcholinesterase inhibitors have with their target, Carotti and co-workers synthesized a large group of coumarin derivatives that provided insight into the structure–activity relationships, some of which proved to be very potent and selective. Gasco and colleagues discuss their work with analogues of the anti-asthmatic drug zileuton in their project aimed at developing multitarget drugs with greater efficacy as vasodilators for the treatment of allergic disorders and asthma. Specific antagonists of the cannabinoid receptor 1 (CB1) could be used to treat obesity and other metabolic disorders, and Shia and colleagues report their work toward a potential lead CB1 inverse agonist.
This month's cluster is focused on research into cancer treatments, and is composed of eight Full Papers. Doyle, Zubieta, and colleagues explored various conjugates between a rhenium chelate and 2'-deoxypyrimidines as potential compounds in the treatment and diagnosis of cancer. In hopes of finding new and better leads for the treatment of hormone-depended breast cancer, Potter et al. synthesized and carried out structural characterizations of a series of dual inhibitors of both aromatase and steroid sulfatase. Given the role of cathepsins L and B in cancer, Giralt and co-workers put these proteases in their crosshairs, and created a library of peptidyl aryl vinyl sulfones as potential cathepsin inhibitors; one compound proved particularly potent and selective for cathepsin L. Irradiate 5-methoxypsoralen with UV-A, and one of the photoproducts produced can stimulate erythroid differentiation in leukemia cells; Dall'Acqua, Gambari, et al. report their characterization of this photoproduct, which may aid the development of leukemia treatments. Wiese and colleagues report their identification of specific breast cancer resistance protein inhibitors, a significant step in the fight against multidrug-resistant cancers. Compounds that disrupt microtubule function hold promise for the treatment of various forms of cancer: Chern and colleagues discuss their work with such compounds, which show antiproliferative activity toward prostate cancer cells.
Browse Issue 09/2010 today!