1196806-30-0Relevant articles and documents
Discovery of Novel Class i Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities
Yao, Yiwu,Tu, Zhengchao,Liao, Chenzhong,Wang, Zhen,Li, Shang,Yao, Hequan,Li, Zheng,Jiang, Sheng
, p. 7672 - 7680 (2015/10/20)
A successful structure-based design of novel cyclic depsipeptides that selectively target class I HDAC isoforms is described. Compound 11 has an IC50 of 2.78 nM for binding to the HDAC1 protein, and the prodrugs 12 and 13 also exhibit promising antiproliferative activities in the nanomolar range against various cancer cell lines. Compounds 12 and 13 show more than 20-fold selectivity toward human cancer cells over human normal cells in comparison with romidepsin (FK228), demonstrating low probability of toxic side effects. In addition, compound 13 exhibits excellent in vivo anticancer activities in a human prostate carcinoma (Du145) xenograft model with no observed toxicity. Thus, prodrug 13 has therapeutic potential as a new class of anticancer agent for further clinical translation.
Total synthesis of largazole-devolution of a novel synthetic strategy
Wang, Bo,Forsyth, Craig J.
experimental part, p. 2873 - 2880 (2010/02/28)
The cyanobacterial isolate largazole embodies a compelling combination of a relatively simple, yet unique cyclic depsipeptide structure with remarkable levels of selective cytotoxicity against cancer cell lines versus nontransformed cells. The unique stru
