Isolation and structural elucidation of the human cancer cell gr

Chemistry: natural resins or derivatives; peptides or proteins; – Peptides of 3 to 100 amino acid residues – Cyclic peptides

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530317, 530328, 530329, C07K 512, C07K 764

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active

056462468

ABSTRACT:
The cytostatic, cyclic peptides; phakellistatin 4, phakellistatin 5, phakellistatin 6, phakellistatin 7, phakellistatin 8 and phakellistatin 9 were isolated from the Western Pacific Ocean sponge Phakellia costata. Structural determination was accomplished by utilizing high-field, 2D-NMR experiments and confirmed by results of FAB-MS/MS studies. The absolute configurations were deduced by analyzing the acid hydrolysates using chiral gas chromatographic analytical techniques. The new cyclic peptides were found to have significant in vitro P388 ED.sub.50 values which range between 0.18 .mu.g/ml and 4.1 .mu.g/ml.

REFERENCES:
Pettit et al., "Isolation of Doastatins 10-15 from the marine mollusc Dollla Auricularia," Tetrahedron, vol. 49, No. 41, pp. 9151-9170. 1993.
Pettit et al., "Isolation and Structure of the Marine Sponge Cell Growth Inhibitory Cyclic Peptide Phakellistatin 1," Journal of Natural Products, vol. 56, No. 2, pp. 260-267. Feb. 1993.

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