4.8 Article

Convenient Method for the Synthesis of a Flexible Cyclic Polyamide for Selective Targeting of c-myb G-quadruplex DNA

Journal

ORGANIC LETTERS
Volume 14, Issue 24, Pages 6126-6129

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/ol302918f

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Funding

  1. 973 Program [2012CB720600, 2012CB720601]

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A convenient efficient method for synthesis of a flexible cyclic polyamide (c beta, 1) was developed through cyclodimerization. Electrospray ionization mass spectrometry and nuclear magnetic resonance results showed that 1 selectively binds to the c-myb G-quadruplex with high affinity, and there was no binding with the ILPR, bcl-2, and c-kit G-quadruplexes. This is the first time that a flexible cyclic polyamide was found to have high selectivity for the c-myb G-quadruplex.

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