68548-50-5Relevant academic research and scientific papers
Addressing cytotoxicity of 1,4-biphenyl amide derivatives: Discovery of new potent and selective 17β-hydroxysteroid dehydrogenase type 2 inhibitors
Gargano, Emanuele Marco,Perspicace, Enrico,Carotti, Angelo,Marchais-Oberwinkler, Sandrine,Hartmann, Rolf W.
, p. 21 - 24 (2015/12/18)
Four different classes of new 17β-hydroxysteroid dehydrogenase type 2 (17β-HSD2) inhibitors were synthesized, in order to lower the cytotoxicity exhibited by the lead compound A, via disrupting the linearity and the aromaticity of the biphenyl moiety. Compounds 3, 4, 7a and 8 displayed comparable or better inhibitory activity and selectivity, as well as a lower cytotoxic effect, compared to the reference compound A. The best compound 4 (IC50 = 160 nM, selectivity factor = 168, LD50 ≈ 25 μM) turned out as new lead compound for inhibition of 17β-HSD2.
Synthesis and antiproliferative activity of novel 4-substituted-phenoxy-benzamide derivatives
Sun, Chi-Yu,Li, Yang-Sheng,Shi, Ai-Long,Li, Ya-Fei,Cao, Rui-Fang,Ding, Huai-Wei,Yin, Qing-Qing,Zhang, Li-Juan,Zheng, Hua-Chuan,Song, Hong-Rui
, p. 1307 - 1310 (2015/12/31)
A series of novel 4-substituted-phenoxy-benzamide derivatives bearing an aryl cycloaliphatic amine moiety were synthesized and evaluated for antiproliferative activity against SW620, HT29 and MGC803 cancer cell lines in vitro. The pharmacological data demonstrated that the majority of target compounds exhibited moderate efficacy in HT29 and MGC803 cell lines. Compound 10c showed promising inhibition of hedgehog (Hh) signaling pathway in an Hh-related assay. In addition, the superposition pattern of 10c showed a good fit for a pharmacophoric model generated by Hh inhibitors and provided a basis for further structural optimization.
Phenoxy phenyl pyrrolidine compounds, compositions and methods of use
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, (2008/06/13)
Pyrrolidone derivatives of the formula: STR1 wherein R is hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl, And Y is hydrogen, saturated or unsaturated hydrocarbon radical up to C4, hydroxyethyl, hydroxypropyl or carboxymethyl. T
