Isolation and structure of the human cancer cell growth inhibito

Details Isolation and structure of the human cancer cell growth inhibito Isolation and structure of the human cancer cell growth inhibito

1994-12-20

1998-09-01

Achutamurthy, Ponnathapura

Chemistry: natural resins or derivatives; peptides or proteins;

Peptides of 3 to 100 amino acid residues

Cyclic peptides

514 11, 514 9, 514 2, C07K 764, A61K 3812

Patent

active

058012222

ABSTRACT:
Two new compounds which may be useful in the treatment of one or more neoplastic diseases through chemotherapy have been isolated from the Western Pacific Ocean marine sponge Phakellia sp. The cyclic octapeptides phakellistatin 10 and phakellistatin 11 are disclosed herein.
As the included data demonstrate, phakellistatin 10 attained an LC.sub.50 of less than 10.sup.-5 M per milliliter against the MDA-MB-435 breast cancer cell line. It also achieved total growth inhibition for two breast cancers and two CNS cancer cell lines at a concentration of less than 10.sup.-6 M per milliliter. The included data for phakellistatin 11 shows a moderately higher level of in vitro activity as shown by an LC.sub.50 of less than 10.sup.-5 M per milliliter against the MDA-MB-435 breast cancer cell line and five other cell lines. It also achieved total growth inhibition for two breast cancers, one CNS cancer, one Ovarian cancer, and one non-small cell lung cancer cell lines at a concentration of less than 10.sup.-7 M per milliliter.

REFERENCES:
Tsula, Tetarahedron, vol. 50, No. 16, pp. 4667-4680, (1994) Pettit et al, urnal of Natural Products, vol. 56, No. 2, pp. 260-267, (Feb. 1993).
Pettit et al, J. Org. Chem., vol. 57, pp. 7217-7220, (1992).
Pettit et al, Bioorganic & Medicinal Chem., vol. 4, No. 17, pp. 2091-2096, (1994).

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