333327-39-2Relevant academic research and scientific papers
Orally active docetaxel analogue: Synthesis of 10-deoxy-10-C-morpholinoethyl docetaxel analogues
Iimura, Shin,Uoto, Kouichi,Ohsuki, Satoru,Chiba, Jun,Yoshino, Toshiharu,Iwahana, Michio,Jimbo, Takeshi,Terasawa, Hirofumi,Soga, Tsunehiko
, p. 407 - 410 (2007/10/03)
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.
