Antineoplastic agents 337. Synthesis of dolastatin 10 structural modifications

George Pettit; J. K. Srirangam; J. Barkoczy; M. D. Williams; K. P M Durkin; M. R. Boyd; R. Bai; E. Hamel; J. M. Schmidt; Jean Chapuis

Antineoplastic agents 337. Synthesis of dolastatin 10 structural modifications

George Pettit, J. K. Srirangam, J. Barkoczy, M. D. Williams, K. P M Durkin, M. R. Boyd, R. Bai, E. Hamel, J. M. Schmidt, Jean Chapuis

Research output: Contribution to journal › Article › peer-review

93 Scopus citations

Abstract

New structural modifications of the marine shell-less mollusk peptide constituent dolastatin 10 (1) have been synthesized, and evaluated against a variety of cancer cell lines and for their ability to inhibit tubulin polymerization. A number of useful structure-activity relationships were uncovered. The most important observation was that the dolaphenine unit of dolastatin 10 could be satisfactorily replaced with a phenethylamine. Peptide 11C, designated auristatin PE, was found to exhibit inhibition of cancer cell growth and tubulin assembly comparable to that of dolastatin 10.

Original language	English (US)
Pages (from-to)	529-544
Number of pages	16
Journal	Anti-Cancer Drug Design
Volume	10
Issue number	7
State	Published - 1995

Keywords

Antineoplastic agents
Dolastatin 10
Structural modifications

ASJC Scopus subject areas

Biochemistry
Oncology
General Biochemistry, Genetics and Molecular Biology
Pharmacology
Drug Discovery
Organic Chemistry

Cite this

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abstract = "New structural modifications of the marine shell-less mollusk peptide constituent dolastatin 10 (1) have been synthesized, and evaluated against a variety of cancer cell lines and for their ability to inhibit tubulin polymerization. A number of useful structure-activity relationships were uncovered. The most important observation was that the dolaphenine unit of dolastatin 10 could be satisfactorily replaced with a phenethylamine. Peptide 11C, designated auristatin PE, was found to exhibit inhibition of cancer cell growth and tubulin assembly comparable to that of dolastatin 10.",

keywords = "Antineoplastic agents, Dolastatin 10, Structural modifications",

author = "George Pettit and Srirangam, {J. K.} and J. Barkoczy and Williams, {M. D.} and Durkin, {K. P M} and Boyd, {M. R.} and R. Bai and E. Hamel and Schmidt, {J. M.} and Jean Chapuis",

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T1 - Antineoplastic agents 337. Synthesis of dolastatin 10 structural modifications

AU - Pettit, George

AU - Srirangam, J. K.

AU - Barkoczy, J.

AU - Williams, M. D.

AU - Durkin, K. P M

AU - Boyd, M. R.

AU - Bai, R.

AU - Hamel, E.

AU - Schmidt, J. M.

AU - Chapuis, Jean

PY - 1995

Y1 - 1995

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AB - New structural modifications of the marine shell-less mollusk peptide constituent dolastatin 10 (1) have been synthesized, and evaluated against a variety of cancer cell lines and for their ability to inhibit tubulin polymerization. A number of useful structure-activity relationships were uncovered. The most important observation was that the dolaphenine unit of dolastatin 10 could be satisfactorily replaced with a phenethylamine. Peptide 11C, designated auristatin PE, was found to exhibit inhibition of cancer cell growth and tubulin assembly comparable to that of dolastatin 10.

KW - Antineoplastic agents

KW - Dolastatin 10

KW - Structural modifications

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AN - SCOPUS:0028826495

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Antineoplastic agents 337. Synthesis of dolastatin 10 structural modifications

Abstract

Keywords

ASJC Scopus subject areas

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