Antineoplastic agents 365. Dolastatin 10 SAR probes

George R. Pettit; Jayaram K. Srirangam; Jozsef Barkoczy; Michael D. Williams; Michael R. Boyd; Ernest Hamel; Robin K. Pettit; Fiona Hogan; Ruoli Bai; Jean Charles Chapuis; Shane C. McAllister; Jean M. Schmidt

Antineoplastic agents 365. Dolastatin 10 SAR probes

George R. Pettit, Jayaram K. Srirangam, Jozsef Barkoczy, Michael D. Williams, Michael R. Boyd, Ernest Hamel, Robin K. Pettit, Fiona Hogan, Ruoli Bai, Jean Charles Chapuis, Shane C. McAllister, Jean M. Schmidt

Pediatric Hematology/Oncology

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

77 Scopus citations

Abstract

The remarkable anticancer drug dolastatin 10 (1a) from the Indian Ocean sea hare Dolabella auricularia is currently undergoing phase I clinical trials. Thirty-eight new structural modifications of this unusual peptide have been synthesized and evaluated against a variety of human and murine cancer cell lines, and for their ability to inhibit tubulin polymerization and vinblastine and GTP binding to tubulin. Dolastatin 10 and one structural modification was found to have antifungal activity, while one other structural modification of the parent compound exhibited antibacterial activity. Some of the new peptides approximated the antineoplastic potency of dolastatin 10, especially those based on replacement of the Doe unit with Met, Phe or an appropriately substituted phenylethylamide.

Original language	English (US)
Pages (from-to)	243-277
Number of pages	35
Journal	Anti-Cancer Drug Design
Volume	13
Issue number	4
State	Published - Jun 1998

Keywords

Antineoplastic agents
Dolastatin 10
Structural modifications

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title = "Antineoplastic agents 365. Dolastatin 10 SAR probes",

abstract = "The remarkable anticancer drug dolastatin 10 (1a) from the Indian Ocean sea hare Dolabella auricularia is currently undergoing phase I clinical trials. Thirty-eight new structural modifications of this unusual peptide have been synthesized and evaluated against a variety of human and murine cancer cell lines, and for their ability to inhibit tubulin polymerization and vinblastine and GTP binding to tubulin. Dolastatin 10 and one structural modification was found to have antifungal activity, while one other structural modification of the parent compound exhibited antibacterial activity. Some of the new peptides approximated the antineoplastic potency of dolastatin 10, especially those based on replacement of the Doe unit with Met, Phe or an appropriately substituted phenylethylamide.",

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

author = "Pettit, {George R.} and Srirangam, {Jayaram K.} and Jozsef Barkoczy and Williams, {Michael D.} and Boyd, {Michael R.} and Ernest Hamel and Pettit, {Robin K.} and Fiona Hogan and Ruoli Bai and Chapuis, {Jean Charles} and McAllister, {Shane C.} and Schmidt, {Jean M.}",

year = "1998",

month = jun,

language = "English (US)",

volume = "13",

pages = "243--277",

journal = "Anti-Cancer Drug Design",

issn = "0266-9536",

publisher = "Cognizant Communication Corporation",

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TY - JOUR

T1 - Antineoplastic agents 365. Dolastatin 10 SAR probes

AU - Pettit, George R.

AU - Srirangam, Jayaram K.

AU - Barkoczy, Jozsef

AU - Williams, Michael D.

AU - Boyd, Michael R.

AU - Hamel, Ernest

AU - Pettit, Robin K.

AU - Hogan, Fiona

AU - Bai, Ruoli

AU - Chapuis, Jean Charles

AU - McAllister, Shane C.

AU - Schmidt, Jean M.

PY - 1998/6

Y1 - 1998/6

N2 - The remarkable anticancer drug dolastatin 10 (1a) from the Indian Ocean sea hare Dolabella auricularia is currently undergoing phase I clinical trials. Thirty-eight new structural modifications of this unusual peptide have been synthesized and evaluated against a variety of human and murine cancer cell lines, and for their ability to inhibit tubulin polymerization and vinblastine and GTP binding to tubulin. Dolastatin 10 and one structural modification was found to have antifungal activity, while one other structural modification of the parent compound exhibited antibacterial activity. Some of the new peptides approximated the antineoplastic potency of dolastatin 10, especially those based on replacement of the Doe unit with Met, Phe or an appropriately substituted phenylethylamide.

AB - The remarkable anticancer drug dolastatin 10 (1a) from the Indian Ocean sea hare Dolabella auricularia is currently undergoing phase I clinical trials. Thirty-eight new structural modifications of this unusual peptide have been synthesized and evaluated against a variety of human and murine cancer cell lines, and for their ability to inhibit tubulin polymerization and vinblastine and GTP binding to tubulin. Dolastatin 10 and one structural modification was found to have antifungal activity, while one other structural modification of the parent compound exhibited antibacterial activity. Some of the new peptides approximated the antineoplastic potency of dolastatin 10, especially those based on replacement of the Doe unit with Met, Phe or an appropriately substituted phenylethylamide.

KW - Antineoplastic agents

KW - Dolastatin 10

KW - Structural modifications

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C2 - 9627667

AN - SCOPUS:7144263706

SN - 0266-9536

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JO - Anti-Cancer Drug Design

JF - Anti-Cancer Drug Design

IS - 4

ER -

Antineoplastic agents 365. Dolastatin 10 SAR probes

Abstract

Keywords

UN SDGs

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