Ontology highlight
ABSTRACT:
SUBMITTER: Zeng X
PROVIDER: S-EPMC7386434 | biostudies-literature | 2010 Mar
REPOSITORIES: biostudies-literature
Zeng Xin X Yin Biaolin B Hu Zheng Z Liao Chenzhong C Liu Jinglei J Li Shang S Li Zheng Z Nicklaus Marc C MC Zhou Guangbiao G Jiang Sheng S
Organic letters 20100301 6
The efficient total synthesis of the natural substance largazole is described. Using this strategy, a small library of largazole analogs was developed. Structure-activity relationship studies suggested that the geometry of the alkene in the side chain is critical. While the largazole's analogues with trans-alkene are potent for the antiproliferative effect, those with cis-alkene are completely inactive. Most importantly, replacement of valine with tyrosine in largazole increased selectivity towa ...[more]