728890-58-2Relevant academic research and scientific papers
Dendritic polypeptide-based nanocarriers for the delivery of therapeutic agents
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Page/Page column 15; 16, (2018/04/25)
Dendritic polypeptides useful for the delivery of therapeutic agents into cells are disclosed, together with their methods of preparation. These dendritic polypeptides serve as carriers of drugs, siRNA, aptamers and plasmid DNA in the treatment of various
Synthesis and biological evaluation of aziridin-1-yl oxime-based vorinostat analogs as anticancer agents
Nikitjuka, Anna,Shestakova, Irina,Romanchikova, Nadezhda,Jirgensons, Aigars
, p. 647 - 657 (2016/01/15)
The suberoyl anilide hydroxamic acid (vorinostat) analogs with the aziridin-1-yl oxime moiety as a possible metal chelating functionality have been synthesized. Their biological activity and stability under physiological conditions have been evaluated. Although some of the synthesized compounds demonstrated high antiproliferative activity against human HT1080 fibrosarcoma (HT1080, IC50 0.3-7.7 μM) comparable to vorinostat (HT1080, IC50 2.4 μM), they showed only weak histone deacetylase inhibition activity in HeLa cell line extracts.
Effects of E/Z configuration of fluoroalkene-containing HDAC inhibitors on selectivity for HDAC isoforms
Chuman, Yoshiro,Ueyama, Mariko,Sano, Satoshi,Wu, Fei,Kiyota, Yuhei,Higashi, Takayoshi,Osada, Satoshi,Sakaguchi, Kazuyasu
, p. 833 - 835 (2013/09/02)
Histone deacetylase (HDAC) inhibitors belong to a new class of potential anticancer agents. It may be possible to reduce some of the toxicity by specifically targeting only the HDAC isoform. Here, stereoisomeric HDAC inhibitors containing fluoroalkene were analyzed for their specificity toward HDAC isoforms. Z-Form 1(Z) showed high affinity to HDACs whereas E-isoform 1(E) had lower affinity to HDAC1 and HDAC4. These data suggested that introduction of alkene with E/Z configuration to HDAC inhibitor can be a new strategy to develop the isoform-selective HDAC inhibitors.
Design and synthesis of non-hydroxamate histone deacetylase inhibitors: Identification of a selective histone acetylating agent
Suzuki, Takayoshi,Matsuura, Azusa,Kouketsu, Akiyasu,Hisakawa, Shinya,Nakagawa, Hidehiko,Miyata, Naoki
, p. 4332 - 4342 (2007/10/03)
A series of suberoylanilide hydroxamic acid (SAHA)-based non-hydroxamates was designed, synthesized, and evaluated for their histone deacetylase (HDAC) inhibitory activity. Among these, methyl sulfoxide 15 inhibited HDACs in enzyme assays and caused hyperacetylation of histone H4 while not inducing the accumulation of acetylated α-tubulin in HCT116 cells.
Thiol-based SAHA analogues as potent histone deacetylase inhibitors
Suzuki, Takayoshi,Kouketsu, Akiyasu,Matsuura, Azusa,Kohara, Arihiro,Ninomiya, Shin-Ichi,Kohda, Kohfuku,Miyata, Naoki
, p. 3313 - 3317 (2007/10/03)
In order to find novel nonhydroxamate histone deacetylase (HDAC) inhibitors, a series of thiol-based compounds modeled after suberoylanilide hydroxamic acid (SAHA) was synthesized, and their inhibitory effect on HDACs was evaluated. Compound 6, in which t
