2381-23-9Relevant articles and documents
King,Smith
, p. 1870,1871 (1965)
Design, synthesis and biological evaluation of new oligopyrrole carboxamides linked with tricyclic DNA-intercalators as potential DNA ligands or topoisomerase inhibitors
David-Cordonnier, Marie-Helene,Hildebrand, Marie-Paule,Baldeyrou, Brigitte,Lansiaux, Amelie,Keuser, Christoph,Benzschawel, Kerstin,Lemster, Thomas,Pindur, Ulf
, p. 752 - 771 (2008/02/13)
In the context of the design and synthesis of minor groove binding and intercalating DNA ligands some new oligopyrrole carboxamides were synthesized. These hybrid molecules (combilexins) possess a variable and conformatively flexible spacer at the N-terminal end. As intercalating tricyclic systems acridone, acridine, anthraquinones and in a special case iminostilbene terminate the N-terminal end of the pyrrole chain. The cytotoxicity was examined by the NCI antitumor screening, furthermore, biophysical as well as biochemical studies were performed in order to get some information about the DNA binding properties and topoisomerase inhibition effect of this new series of molecules.
Practical routes to the triarylsulfonyl chloride intermediate of a β3 adrenergic receptor agonist
Ikemoto, Norihiro,Liu, Jinchu,Brands, Karel M.J.,McNamara, James M.,Reider, Paul J.
, p. 1317 - 1325 (2007/10/03)
A β3 adrenergic receptor agonist was prepared on a multi-kilogram scale in high yield and purity via a convergent synthesis. A key intermediate in this synthesis was an arylthiazolylbenzenesulfonyl chloride. The triaryl segment of this sulfonyl chloride was assembled at the thiazole ring via coupling of α-haloketone and thiobenzamide precursors (Hantzsch synthesis). Three strategies for introducing the para-sulfonyl chloride moiety were developed and evaluated. The sulfonation/chlorination and diazotization/chlorosulfonylation routes were found the most efficient.