195317-10-3Relevant articles and documents
Cationic pentaheteroaryls as selective G-quadruplex ligands by solvent-free microwave-assisted synthesis
Petenzi, Michele,Verga, Daniela,Largy, Eric,Hamon, Florian,Doria, Filippo,Teulade-Fichou, Marie-Paule,Guédin, Aurore,Mergny, Jean-Louis,Mella, Mariella,Freccero, Mauro
, p. 14487 - 14496 (2012)
We report herein a solvent-free and microwaved-assisted synthesis of several water soluble acyclic pentaheteroaryls containing 1,2,4-oxadiazole moieties (1-7). Their binding interactions with DNA quadruplex structures were thoroughly investigated by FRET melting, fluorescent intercalator displacement assay (G4-FID) and CD spectroscopy. Among the G-quadruplexes considered, attention was focused on telomeric repeats together with the proto-oncogenic c-kit sequences and the c-myc oncogene promoter. Compound 1, and to a lesser extent 2 and 5, preferentially stabilise an antiparallel structure of the telomeric DNA motif, and exhibit an opposite binding behaviour to structurally related polyoxazole (TOxaPy), and do not bind duplex DNA. The efficiency and selectivity of the binding process was remarkably controlled by the structure of the solubilising moieties. Copyright
1-aziridino-1-hydroxyiminomethyl-derivates, method for the production thereof and medicaments containing said compounds
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Page/Page column 5-6, (2008/06/13)
Described are new 1-aziridino-1-hydroxyiminomethyl derivatives with the general formula (I), wherein R is able to is a single bond or a linker moiety capable of covalently bonding two aziridine oxime groups, R1 and R2 independently of one another are selected from the group consisting of —H, —CH3, —C2H5, —CN, —COOH, —COOCH3, —COOC2H5, —CONH2, or —C6H5 group, and n is the whole number 2, provided that R1 and R2 are not both —H and provided that R1 is not —H if R2 is —CH3 and R1 is not —CH3 if R2 is —H The compounds of general formula (I) show antitumor activity.
