Journal
JOURNAL OF NATURAL PRODUCTS
Volume 74, Issue 5, Pages 1003-1008Publisher
AMER CHEMICAL SOC
DOI: 10.1021/np100877h
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Funding
- Division of Cancer Treatment and Diagnosis, NCI, DHHS [RO1 CA 90441-02-05, 2R56-CA 090441-06A1, 5R01 CA 090441-07]
- Arizona Disease Control Research Commission
- J. W. Kieckhefer Foundation
- Margaret T. Morris Foundation
- Robert B. Dalton Endowment Fund
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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.
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