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Synthetic Analogues of the Microtubule-Stabilizing Agent (+)-Discodermolide: Preparation and Biological Activity
| Title: | Synthetic Analogues of the Microtubule-Stabilizing Agent (+)-Discodermolide: Preparation and Biological Activity. |
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| Name(s): |
Gunasekera, Sarath P., creator Mickel, Stuart J., creator Daeffler, Robert, creator Niederer, Daniel, creator Wright, Amy E., creator Linley, P. A., creator Pitts, Tara P., creator |
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| Type of Resource: | text | |
| Genre: | Article | |
| Issuance: | single unit | |
| Date Issued: | 2004 | |
| Publisher: | American Chemical Society and American Society of Pharmacognosy | |
| Extent: | 9 p. | |
| Physical Description: | ||
| Language(s): | English | |
| Identifier: | 3164107 (digitool), FADT3164107 (IID), fau:5610 (fedora), 10.1021/np030493w (doi) | |
| Note(s): |
A series of seven synthetic discodermolide analogues 2-8, which are minor side products generated during the final stages in the synthesis of (+)-discodermolide (1), have been purified and evaluated for in vitro cytotoxicity against A549, P388, MFC-7, NCI/ADR, PANC-1, and VERO cell lines. These synthetic analogues showed a significant variation of cytotoxicity and confirmed the importance of the C-7 hydroxy through C-17 hydroxy molecular fragment for potency. Specifically, these analogues suggested the relevance of the C-11 hydroxyl group, the C-13 double bond, and the C-16 (S) stereochemistry for the potency of (+)-discodermolide. This document is the accepted manuscript version of a published work that appeared in final form in Journal of Natural Products after peer review and technical editing by the publisher. To access the final edited and published work see http://dx.doi.org/10.1021/np030493w. This article may be cited as: Gunasekera, S. P., Mickel, S. J., Daeffler, R., Niederer, D., Wright, A. E., Linley, P. & Pitts, T. (2004). Synthetic Analogues of the Microtubule-Stabilizing Agent (+)-Discodermolide: Preparation and Biological Activity. Journal of Natural Products, 67(5), 749-756. Florida Atlantic University. Harbor Branch Oceanographic Institute contribution #1544. |
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| Subject(s): |
Microtubules Cancer --Research Biopharmaceutics Molecular biology Stereochemistry |
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| Persistent Link to This Record: | http://purl.flvc.org/FCLA/DT/3164107 | |
| Links: | http://dx.doi.org/10.1021/np030493w | |
| Restrictions on Access: | ©2004 American Chemical Society and American Society of Pharmacognosy | |
| Host Institution: | FAU |
