65623-97-4Relevant academic research and scientific papers
HDAC-Bax Multiple Ligands Enhance Bax-Dependent Apoptosis in HeLa Cells
Liang, Tao,Zhou, Yi,Elhassan, Reham M.,Hou, Xuben,Yang, Xinying,Fang, Hao
, p. 12083 - 12099 (2020/11/02)
Inspired by the synergistic effect of BTSA1 (a Bax activator) and SAHA (a histone deacetylase (HDAC) inhibitor) in HeLa cell growth suppression, a series of novel HDAC-Bax multiple ligands were designed rationally. Compound 23, which possesses similar HDAC inhibitory activity relative to SAHA and Bax affinity comparable to BTSA1, exhibits a superior growth suppression against HeLa cells, and its antiproliferative activities are 15-fold and 3-fold higher than BTSA1 and SAHA, respectively. The better antiproliferative activity and lower cytotoxicity of compound 23 indicated that our HDAC-Bax multiple ligand design strategy achieved success. Further studies suggested that compound 23 could enhance Bax-dependent apoptosis by upregulating Bax, followed by inducing the conformational activation of Bax. To our knowledge, we first report HDAC-Bax multiple ligands and demonstrate a new paradigm for the treatment of solid tumors by enhancing Bax-dependent apoptosis.
Substituted phenylacetic acid compounds and process for preparation thereof
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, (2008/06/13)
Substituted phenylacetic acid compounds represented by the following general formula and preparation thereof: STR1 wherein R1 is hydrogen or protected carboxy, R2 is hydrogen, or protected amino, provided that when R1 is h
