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

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.
AuthorsS Iimura, K Uoto, S Ohsuki, J Chiba, T Yoshino, M Iwahana, T Jimbo, H Terasawa, T Soga
JournalBioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 11 Issue 3 Pg. 407-10 (Feb 12 2001) ISSN: 0960-894X [Print] England
PMID11212122 (Publication Type: Journal Article)
Chemical References
  • 10-deoxy-10-C-morpholinoethyl docetaxel
  • Antineoplastic Agents, Phytogenic
  • Morpholines
  • Taxoids
  • Docetaxel
  • Paclitaxel
Topics
  • Administration, Oral
  • Animals
  • Antineoplastic Agents, Phytogenic (administration & dosage, chemical synthesis, pharmacology)
  • Cell Division (drug effects)
  • Combinatorial Chemistry Techniques
  • Docetaxel
  • Drug Screening Assays, Antitumor
  • Humans
  • Inhibitory Concentration 50
  • Lung Neoplasms (drug therapy, pathology)
  • Melanoma, Experimental (drug therapy)
  • Mice
  • Mice, Inbred C57BL
  • Morpholines (administration & dosage, chemical synthesis, pharmacology)
  • Paclitaxel (administration & dosage, analogs & derivatives, chemical synthesis, pharmacology)
  • Solubility
  • Structure-Activity Relationship
  • Survival Rate
  • Taxoids
  • Tumor Cells, Cultured (drug effects)

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