Abstract
Three advances necessary to bring dolastatin 16 (1) into full-scale preclinical development as an anticancer drug have been accomplished. The X-ray crystal structure of dolastatin 16 has been solved, which allowed stereoselective syntheses of its two new amino acid units, dolamethylleuine (Dml) and dolaphenvaline (Dpv), to be completed. The X-ray crystal structures of synthetic Z-Dml and TFA-Dpv have also been completed. (Chemical Equation Presented).
| Original language | English (US) |
|---|---|
| Pages (from-to) | 1003-1008 |
| Number of pages | 6 |
| Journal | Journal of Natural Products |
| Volume | 74 |
| Issue number | 5 |
| DOIs | |
| State | Published - May 27 2011 |
ASJC Scopus subject areas
- Analytical Chemistry
- Molecular Medicine
- Pharmacology
- Pharmaceutical Science
- Drug Discovery
- Complementary and alternative medicine
- Organic Chemistry
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Dive into the research topics of 'Antineoplastic agents. 590. X-ray crystal structure of dolastatin 16 and syntheses of the dolamethylleuine and dolaphenvaline units'. Together they form a unique fingerprint.Datasets
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CCDC 801990: Experimental Crystal Structure Determination
Pettit, G. R. (Contributor), Smith, T. H. (Contributor), Xu, J. (Contributor), Herald, D. L. (Contributor), Flahive, E. J. (Contributor), Anderson, C. R. (Contributor), Belcher, P. E. (Contributor), Knight, J. C. (Contributor) & Pettit, G. R. (Contributor), The Cambridge Structural Database, 2011
DOI: 10.5517/ccvxjnx, http://www.ccdc.cam.ac.uk/services/structure_request?id=doi:10.5517/ccvxjnx&sid=DataCite
Dataset
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CCDC 801992: Experimental Crystal Structure Determination
Pettit, G. R. (Contributor), Smith, T. H. (Contributor), Xu, J. (Contributor), Herald, D. L. (Contributor), Flahive, E. J. (Contributor), Anderson, C. R. (Contributor), Belcher, P. E. (Contributor), Knight, J. C. (Contributor) & Pettit, G. R. (Contributor), The Cambridge Structural Database, 2011
DOI: 10.5517/ccvxjqz, http://www.ccdc.cam.ac.uk/services/structure_request?id=doi:10.5517/ccvxjqz&sid=DataCite
Dataset
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CCDC 801991: Experimental Crystal Structure Determination
Pettit, G. R. (Contributor), Smith, T. H. (Contributor), Xu, J. (Contributor), Herald, D. L. (Contributor), Flahive, E. J. (Contributor), Anderson, C. R. (Contributor), Belcher, P. E. (Contributor), Knight, J. C. (Contributor) & Pettit, G. R. (Contributor), The Cambridge Structural Database, 2011
DOI: 10.5517/ccvxjpy, http://www.ccdc.cam.ac.uk/services/structure_request?id=doi:10.5517/ccvxjpy&sid=DataCite
Dataset