Author/Authors :
Shin Iimura، نويسنده , , Kouichi Uoto، نويسنده , , Satoru Ohsuki، نويسنده , , Jun Chiba، نويسنده , , Toshiharu Yoshino، نويسنده , , Michio Iwahana، نويسنده , , Takeshi Jimbo، نويسنده , , Hirofumi Terasawa، نويسنده , , Tsunehiko Soga، نويسنده ,
Abstract :
To improve cytotoxicity of 10-deoxy-10-C-morpholinoethyl docetaxel analogues against various tumor cell lines including resistant cells expressing P-glycoprotein (P-gp), we modified the 7-hydroxyl group to hydrophobic groups (methoxy, deoxy, 6,7-olefin, α-F, 7-β-8-β-methano, fluoromethoxy). Among these analogues, the 7-methoxy analogue showed the strongest cytotoxicity. This analogue showed potent activity against B16 melanoma BL6 in vivo by oral administration.
