Document Detail

Relationships between the structure of taxol analogues and their antimitotic activity.
MedLine Citation:
PMID:  1672159     Owner:  NLM     Status:  MEDLINE    
A variety of synthetic analogues of taxol, a naturally occurring antitumor diterpene, were examined for their potency to inhibit microtubule disassembly. For some of the compounds, the in vitro cytotoxic properties showed a good correlation with the tubulin assay. This structure-activity relationship study shows that inhibition of microtubule disassembly is quite sensitive to the configuration at C-2' and C-3'. A correlation between the conformation of the side chain at C-13 and the activity is suggested. Of all the compounds examined, one of the most potent in inhibiting microtubule disassembly and in inhibiting murine P388 leukemic cells, N-debenzoyl-N-tert-(butoxycarbonyl)-10-deacetyltaxol, named taxotere, was selected for evaluation as a potential anticancer agent.
F Guéritte-Voegelein; D Guénard; F Lavelle; M T Le Goff; L Mangatal; P Potier
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  34     ISSN:  0022-2623     ISO Abbreviation:  J. Med. Chem.     Publication Date:  1991 Mar 
Date Detail:
Created Date:  1991-04-17     Completed Date:  1991-04-17     Revised Date:  2008-11-21    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  992-8     Citation Subset:  IM    
Institut de Chimie des Substances Naturelles, Centre National de la Recherche Scientifique, Gif-sur-Yvette, France.
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MeSH Terms
Alkaloids / chemistry*,  pharmacology
Antineoplastic Agents / chemistry*,  pharmacology
Brain / ultrastructure
Cell Division / drug effects
Chemical Phenomena
Leukemia P388 / pathology
Microtubules / drug effects,  metabolism
Molecular Conformation
Molecular Structure
Structure-Activity Relationship
Tubulin / metabolism
Reg. No./Substance:
0/Alkaloids; 0/Antineoplastic Agents; 0/Tubulin; 33069-62-4/Paclitaxel

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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