AUTOFLUORESCENT FUSED-PYRIMIDINE NUCLEOSIDES: SYNTHESIS AND EVALUATION AS PERMEANTS AND INHIBITORS OF HUMAN NUCLEOSIDE TRANSPORTERS.

Autor: Nowak, Ireneusz, Damaraju, Vijaya I., Cass, Carol E., Young, James D., Robinsa, Morris J.
Předmět:
Zdroj: Collection of Czechoslovak Chemical Communications; 2011, Vol. 76 Issue 12, p1395-1412, 18p, 1 Color Photograph, 4 Diagrams, 1 Chart, 1 Graph
Abstrakt: Nucleosides with an aromatic five-membered ring heterocycle (N, O, or S) fused at C4-C5 of pyrimidin-2-one were prepared by ring closures with 5-(alkyn-1-yl)pyrimidin-2-one intermediates, heterocyclic atom replacements, and ring closure with a 5-aminocytidine derivative. Ultraviolet absorption and emission properties of the autofluorescent products enabled studies on permeation and inhibition of the trans-cellular trafficking effected by human equilibrative nucleoside transporters (hENTs). Some of the autofluorescent nucleosides were shown to be potent and selective inhibitors of human concentrative nucleoside transporters (hCNTs) in a companion study reported elsewhere. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index