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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Authors | S Iimura, K Uoto, S Ohsuki, J Chiba, T Yoshino, M Iwahana, T Jimbo, H Terasawa, T Soga |
Journal | Bioorganic & medicinal chemistry letters
(Bioorg Med Chem Lett)
Vol. 11
Issue 3
Pg. 407-10
(Feb 12 2001)
ISSN: 0960-894X [Print] England |
PMID | 11212122
(Publication Type: Journal Article)
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Chemical References |
- 10-deoxy-10-C-morpholinoethyl docetaxel
- Antineoplastic Agents, Phytogenic
- Morpholines
- Taxoids
- Docetaxel
- Paclitaxel
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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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