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Design and synthesis of C6-C8 bridged epothilone A.

ABSTRACT: A conformationally restrained epothilone A analogue (3) with a short bridge between methyl groups at C6 and C8 was designed and synthesized. Preliminary biological evaluation indicates 3 to be only weakly active (IC50 = 8.5 microM) against the A2780 human ovarian cancer cell line.

SUBMITTER: Zhan W 

PROVIDER: S-EPMC3249659 | biostudies-literature | 2008 Apr

REPOSITORIES: biostudies-literature

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Design and synthesis of C6-C8 bridged epothilone A.

Zhan Weiqiang W   Jiang Yi Y   Brodie Peggy J PJ   Kingston David G I DG   Liotta Dennis C DC   Snyder James P JP  

Organic letters 20080321 8

A conformationally restrained epothilone A analogue (3) with a short bridge between methyl groups at C6 and C8 was designed and synthesized. Preliminary biological evaluation indicates 3 to be only weakly active (IC50 = 8.5 microM) against the A2780 human ovarian cancer cell line. ...[more]

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