Antineoplastic agents 337. Synthesis of dolastatin 10 structural modifications.
Anticancer Drug Des
; 10(7): 529-44, 1995 Oct.
Article
in En
| MEDLINE
| ID: mdl-7495477
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.
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Collection:
01-internacional
Database:
MEDLINE
Main subject:
Oligopeptides
/
Antineoplastic Agents
Limits:
Animals
/
Humans
Language:
En
Journal:
Anticancer Drug Des
Journal subject:
ANTINEOPLASICOS
/
FARMACOLOGIA
Year:
1995
Document type:
Article
Affiliation country:
United States