Bis-indole derivatives with antitumor activity turn out to be specific ligands of human telomeric G-quadruplex
نویسندگان
چکیده
Bis-indolinone derivatives having either 2,6-disubstituted pyridine core (1a and 1b) or 1,10-disubstituted phenanthroline core (2a and 2b), already known to have antitumor activity, have been tested as potential G-quadruplex binders. Compounds 2a and 2b are able to selectively stabilize G-quadruplex over duplex DNA, and also to discriminate among different G-quadruplex structures, having a particular affinity for the parallel form of the human telomeric G-quadruplex. Both compounds are also able to induce telomeric DNA damage that may explain the activity of these compounds.
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عنوان ژورنال:
دوره 2 شماره
صفحات -
تاریخ انتشار 2014