| Literature DB >> 7495477 |
G R Pettit1, J K Srirangam, J Barkoczy, M D Williams, K P Durkin, M R Boyd, R Bai, E Hamel, J M Schmidt, J C Chapuis.
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.Entities:
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Year: 1995 PMID： 7495477
Source DB: PubMed Journal: Anticancer Drug Des ISSN： 0266-9536