457-52-3Relevant academic research and scientific papers
Selective HDAC inhibitors with potent oral activity against leukemia and colorectal cancer: Design, structure-activity relationship and anti-tumor activity study
Li, Xiaoyang,Zhang, Yingjie,Jiang, Yuqi,Wu, Jingde,Inks, Elizabeth S.,Chou, C. James,Gao, Shuai,Hou, Jinning,Ding, Qinge,Li, Jingyao,Wang, Xue,Huang, Yongxue,Xu, Wenfang
, p. 185 - 206 (2017)
Previously, we reported the discovery of a series of N-hydroxycinnamamide-based HDAC inhibitors, among which compound 11y exhibited high HDAC1/3 selectivity. In this current study, structural derivatization of 11y led to a new series of benzamide based HDAC inhibitors. Most of the compounds exhibited high HDACs inhibitory potency. Compound 11a (with 4-methoxybenzoyl as N-substituent in the cap and 4-(aminomethyl) benzoyl as the linker group) exhibited selectivity against HDAC1 to some extent, and showed potent antiproliferative activity against several tumor cell lines. In?vivo studies revealed that compound 11a displayed potent oral antitumor activity in both hematological tumor cell U937 xenograft model and solid tumor cell HCT116 xenograft model with no obvious toxicity. Further modification of benzamide 3, 11a and 19 afforded new thienyl and phenyl compounds (50a, 50b, 63a, 63b and 63c) with dramatic HDAC1 and HDAC2 dual selectivity, and the fluorine containing compound 56, with moderate HDAC3 selectivity.
Synthesis and anticonvulsant activity of new 2,3-benzodiazepines as AMPA receptor antagonists
De Sarro, Angela,De Sarro, Giovambattista,Gitto, Rosaria,Grasso, Silvana,Micale, Nicola,Zappala, Maria
, p. 178 - 187 (2007/10/03)
Novel 1-aryl-3,5-dihydro-7,8-methylenedioxy-4H-2,3-benzodiazepin-4-ones (12a-j) were prepared and their anticonvulsant effects were evaluated by using various models of experimental epilepsy. The seizures were evoked both by means of auditory stimulation
Synthesis and structure-activity relationships of 2- pyrazinylcarboxamidobenzoates and β-ionylideneacetamidobenzoates with retinoidal activity
Jones, Paul,Villeneuve, Gérald B.,Fei, Chengpei,DeMarte, Josie,Haggarty, Allison J.,Nwe, Khin Than,Martin, Deborah A.,Lebuis, Anne-Marie,Finkelstein, Joshua M.,Gour-Salin, Barbara J.,Chan, Tak Hang,Leyland-Jones, Brian R.
, p. 3062 - 3077 (2007/10/03)
The structure-activity relationships of two series of novel retinoids (2-pyrazinylcarboxamidobenzoates and β-ionylideneacetamidobenzoates) have been investigated by evaluating their ability to induce differentiation in both human promyelocytic leukemia (H
