2. Academic Validation
  3. Orally active docetaxel analogue: synthesis of 10-deoxy-10-C-morpholinoethyl docetaxel analogues

Orally active docetaxel analogue: synthesis of 10-deoxy-10-C-morpholinoethyl docetaxel analogues

  • Bioorg Med Chem Lett. 2001 Feb 12;11(3):407-10. doi: 10.1016/s0960-894x(00)00682-x.
S Iimura 1,  K Uoto,  S Ohsuki,  J Chiba,  T Yoshino,  M Iwahana,  T Jimbo,  H Terasawa,  T Soga
Affiliations

Affiliation

  • 1 New Product Research Laboratories IV, Daiichi Pharmaceutical Co., Ltd., Tokyo, Japan.
PMID: 11212122 DOI: 10.1016/s0960-894x(00)00682-x
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, alpha-F, 7-beta-8-beta-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.

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