Three new antineoplastic glycosides, phyllanthostatins 1 (2a), 2 (2c), and 3 (3a), as well as phyllanthoside (2b), have been isolated from the Central American tree Phyllanthus acuminatus Vahl. The phyllanthostatins 1 (2a), 2 (2c), and 3 (3a) and phyllanthoside (2b) structures were completely assigned by detailed analyses of spectral data (principally by 400-MHz NMR) and have been confirmed by X-ray crystallographic analyses of degradation products. In addition to inhibiting growth of the murine P388 lymphocytic leukemia, both phyllanthostatin 1 and phyllanthoside were found to markedly retard progression of the murine B16 melanoma. One of these unique glycosides, phyllanthoside (2b), is in preclinical development at the U.S. National Cancer Institute.
ASJC Scopus subject areas
- Organic Chemistry