Synthesis and evaluation of paclitaxel C7 derivatives: Solution phase synthesis of combinatorial libraries

A novel and efficient two-step, automated solution phase synthesis of a 26-membered combinatorial chemistry library of paclitaxel C7 esters was accomplished using the HP 7686 Solution Phase Synthesizer. Results of combinatorial synthesis, purification, analysis, and biological evaluation are describ...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1998-11, Vol.8 (22), p.3181-3186
Main Authors: Bhat, Laxminarayan, Liu, Yanbin, Victory, Sam F., Himes, Richard H., Georg, Gunda I.
Format: Article
Language:English
Subjects:
Antineoplastic agents
Antineoplastic Agents, Phytogenic - chemical synthesis
Antineoplastic Agents, Phytogenic - pharmacology
Biological and medical sciences
General aspects
Humans
Medical sciences
Paclitaxel - analogs & derivatives
Paclitaxel - pharmacology
Pharmacology. Drug treatments
Structure-Activity Relationship
Tumor Cells, Cultured
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Summary:A novel and efficient two-step, automated solution phase synthesis of a 26-membered combinatorial chemistry library of paclitaxel C7 esters was accomplished using the HP 7686 Solution Phase Synthesizer. Results of combinatorial synthesis, purification, analysis, and biological evaluation are described. A novel and efficient two-step, automated solution-phase synthesis of a 26-membered combinatorial chemistry library of paclitaxel C7 esters was accomplished using the HP 7686 Solution Phase Synthesizer. Results of combinatorial synthesis, purification, analysis, and biological evaluation are described.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(98)00551-4