کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
5219235 | 1503210 | 2012 | 5 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Synthesis of bisquinoline-pyrrole oligoamide as G-quadruplex binding ligand Synthesis of bisquinoline-pyrrole oligoamide as G-quadruplex binding ligand](/preview/png/5219235.png)
A one-pot procedure using ammonium formate under palladium catalysis for the reductive dechlorination and reduction of nitro group of 4-chloro-8-nitro-quinoline derivatives has be successfully carried out. This has lead to the synthesis of bisquinoline-pyrrole oligoamide 1, which show significant G-quadruplex selectivity in preference to duplex DNA. The cooperativity between the bisquinoline and pyrrole oligoamide moieties for good binding affinity to G-quadruplex was proven by synthesizing 2 and 3 lacking a quinoline ring and pyrrole amide, respectively, and both show much reduce affinity to G-quadruplex. Altogether, the results demostrate that the appropriate combination of two chromophores to form the hybride can attenuate binding affinity and selectivity towards G-quadruplex, an important criteria for the rational drug design.
Journal: Tetrahedron - Volume 68, Issues 27â28, 8 July 2012, Pages 5453-5457