Author/Authors :
Raghuram S. Tangirala، نويسنده , , Rachel Dixon، نويسنده , , Danzhou Yang، نويسنده , , Attila Ambrus، نويسنده , , Smitha Antony، نويسنده , , Keli Agama، نويسنده , , Yves Pommier، نويسنده , , Dennis P. Curran، نويسنده ,
Abstract :
Both enantiomers of 20-fluorocamptothecin and the racemate have been prepared by total synthesis. The (R)-enantiomer is essentially inactive in a topoisomerase-I/DNA assay, while the (S)-enantiomer is much less active than (20S)-camptothecin. The lactone ring of 20-fluorocamptothecin hydrolyzes more rapidly than that of camptothecin in PBS. The results provide insight into the role of the 20-hydroxy group in the binding of camptothecin to topoisomerase-I and DNA.
