Author/Authors :
Liu، نويسنده , , Changhui and Tamm، نويسنده , , Markus and Nِtzel، نويسنده , , Marcus W. and de Meijere، نويسنده , , Armin and Schilling، نويسنده , , Jennifer K. and Kingston، نويسنده , , David G.I.، نويسنده ,
Abstract :
Four paclitaxel analogs with a cyclopropanated side-chain were synthesized by coupling of the spirocyclopropanated oxazoline-5-carboxylic acid 4 with 7-TES-baccatin III, followed by hydrolytic ring opening and rearrangement. The absolute configuration of the 2′-position was determined by NMR analysis of the corresponding Mosher esters. The two new paclitaxel analogs with the R configuration at C-2′ were both active in the A2780 mammalian cell line cytotoxicity assay, but much less than paclitaxel itself.
