Dolastatin 15 derivatives

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai

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514 2, 514 17, 530328, 530329, 530330, A61K 3800

Patent

active

061437212

ABSTRACT:
Compounds of the present invention include cell growth inhibitors which are peptides of Formula I,

REFERENCES:
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patent: 5502032 (1996-03-01), Haupt et al.
patent: 5504191 (1996-04-01), Pettit et al.
patent: 5530097 (1996-06-01), Pettit et al.
patent: 5554725 (1996-09-01), Pettit
patent: 5807984 (1998-09-01), Kling et al.
patent: 5831002 (1998-11-01), Haupt et al.
Pettit, G.R., et al., "The Isolation and Structure of a Remarkable Marine Animal Antineoplastic Constituent: Dolastatin 10," J. Am. Chem. Soc. 109:6883-6885 (1987).
Bai, R., et al., "Structure-Activity Studies with Chiral Isomers and With Segments of the Antimitotic Marine Peptide Dolastatin 10," Biochemical Pharmacology 40(8):1859-1864 (1990).
Pettit, G.R., et al., "Antineoplastic Agents. 220. Synthesis of Natural (-)-Dolastatin 15," J. Am. Chem. Soc., 113:6692-6693 (1991).
Bai, R., et al., "Dolastatin 15, a potent antimitotic depsipeptide derived from Dolabella auricularia. Interaction with tubulin and effects on cellular microtubules," 1-Pharmacology Abstract 117: 10373g p. 41 (1992).
Pettit, G.R., et al., "Isolation and Structure of the Cytostatic Depsipeptide Dolastatin 13 from the Sea Hare Dolabella auricularia," J. Am. Chem. Soc., 111(13):5015-5017 (1989).
Pettit, G.R., et al., "Antineoplastic Agents 337. Synthesis of Dolastatin-10 Structural Modifications," Anti-Cancer Drug Design, 10:529-544 (1995).
Miyazaki, K., et al., "Synthesis and Antitumor Activity of Novel Dolastatin-10 Analogs," Chem. Pharm. Bull., 43(10):1706-1718 (1995).
Pettit, G.R., et al.,"Isolation and Structure of the Cytostatic Linear Depsipeptide Dolastatin 15," J. Org. Chem., 54:6005-6006 (1989).
Pettit, G.R., et al., "The Dolastatins 20. A Convenient Synthetic Route to Dolastatin 15," Tetrahedron, 50(42):12097-12108 (1994).
Pettit, G.R., et al., Isolation of Dolastatins 10-15 from the Marine Mollusc Dolabella Auricularia, Tetrahedron, 49(42):9151-9170 (1993).

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