Synthesis and bioactivity of 2,4-diacyl analogues of paclitaxel
The 2,4-diacyl paclitaxel analogues 8a– 8r were prepared from paclitaxel by acylation of 4-deacetyl-2-debenzoylpaclitaxel 1,2-carbonate ( 3 ) followed either by hydrolysis of the carbonate and acylation or by direct treatment of the carbonate with an aryllithium. Some of the resulting derivatives sh...
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Published in | Bioorganic & medicinal chemistry Vol. 9; no. 1; pp. 171 - 178 |
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Main Authors | , , , , , , , |
Format | Journal Article |
Language | English |
Published |
Oxford
Elsevier Ltd
2001
Elsevier Science |
Subjects | |
Online Access | Get full text |
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Summary: | The 2,4-diacyl paclitaxel analogues
8a–
8r were prepared from paclitaxel by acylation of 4-deacetyl-2-debenzoylpaclitaxel 1,2-carbonate (
3
) followed either by hydrolysis of the carbonate and acylation or by direct treatment of the carbonate with an aryllithium. Some of the resulting derivatives showed significantly improved tubulin assembly activity and cytotoxicity as compared with paclitaxel; in some cases this improvement was especially significant for paclitaxel-resistant cell lines. |
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Bibliography: | ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23 |
ISSN: | 0968-0896 1464-3391 |
DOI: | 10.1016/S0968-0896(00)00233-9 |