کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
5221489 | 1383421 | 2010 | 9 صفحه PDF | دانلود رایگان |
New conceivable synthetic approach for the construction of nitrogen-rich 1,2,3-triazolo-pyrrolo[2,1-c][1,4]benzodiazepine (TPBD, 3a-c) trimers has been developed. The first example of a bis-1,2,3-triazolo-bridged unsymmetrical PBD trimer has been successfully synthesized by employing a CuAAC type 'click' chemistry protocol. This efficient route generates tri-imine functionality in a single molecule. It has been envisaged that such tri-imine functionalities could bring in efficient interaction with DNA in a sequence-selective manner in the minor groove of duplex DNA. One of the representative analogues 3c has shown improved DNA-binding ability (ÎTm 23.7 °C) by thermal denaturation studies using CT-DNA and this data is also supported by molecular modeling (MD) studies.
Journal: Tetrahedron - Volume 66, Issue 29, 17 July 2010, Pages 5498-5506