Chiral discrimination in binding of enantiomers of 2-(aminoalkoxy)-substituted 4-(2-thienyl)pyrimidines and 4,6-bis(2-thienyl)pyrimidines with duplex DNA |
| |
Authors: | Strekowski Lucjan Cegla Marek T Honkan Vidya Buczak Henryk Winkeljohn W Rucks Baumstark Alfons L Wilson W David |
| |
Institution: | Department of Chemistry, Georgia State University, Atlanta, 0302-4098, USA. lucjan@gsu.edu |
| |
Abstract: | Thienylpyrimidines substituted at position 2 of the pyrimidine with a chiral aminoalkoxy group were synthesized. Upon interaction with duplex DNA, the unfused heteroaromatic system of these compounds intercalates with DNA base pairs and the protonated side chain is located in the major groove. The S-enantiomers bind more strongly than their R-counterparts with enantiomeric discrimination, as measured by a ratio of binding constants K(S)/K(R), ranging from 1.2 to 2.4. |
| |
Keywords: | |
本文献已被 ScienceDirect PubMed 等数据库收录! |
|