62208-63-3Relevant articles and documents
NOTCH INHIBITORS AND USES THEREOF
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Paragraph 0811-0813, (2021/11/26)
Disclosed herein, inter alia, are compounds for inhibiting Notch and uses thereof.
Design, synthesis and biological evaluation of piperazino-enaminones as novel suppressants of pro-Inflammatory cytokines
Ghoneim, Ola M.,Bill, Ashley,Dhuguru, Jyothi,Szollosi, Doreen E.,Edafiogho, Ivan O.
, p. 3890 - 3898 (2018/06/14)
Infection triggers the release of pro-inflammatory cytokines (TNF-alpha and IL-6). Over-production, however, cause tissue injury seen in severe asthma. The ability of enaminone E121 to reduce pro-inflammatory cytokines in our laboratory encouraged further examination of its structural scaffold. Piperazino-enaminones were designed by incorporating n-arylpiperazine motif into the aromatic enaminone. Four possible modifications were explored systematically. Synthesis was accomplished by amination of the corresponding methyl/ethyl 2,4-dioxo-6-(substituted)cyclohexane-carboxylate. Sixteen novel compounds were synthesized. Biological activity was tested in J774 macrophages stimulated with lipopolysaccharides. The release of cytokines was measured via ELISA. Four compounds significantly suppressed TNF-alpha and IL-6 release in dose-dependent manner.
Synthesis of benzimidazoles via iridium-catalyzed acceptorless dehydrogenative coupling
Sun, Xiang,Lv, Xiao-Hui,Ye, Lin-Miao,Hu, Yu,Chen, Yan-Yan,Zhang, Xue-Jing,Yan, Ming
supporting information, p. 7381 - 7383 (2015/07/15)
Iridium-catalyzed acceptorless dehydrogenative coupling of tertiary amines and arylamines has been developed. A number of benzimidazoles were prepared in good yields. An iridium-mediated C-H activation mechanism is suggested. This finding represents a novel strategy for the synthesis of benzimidazoles.