1064448-86-7Relevant academic research and scientific papers
Synthesis of resveratrol acrylamides derivatives and biological evaluation of their anti-proliferative effect on cancer cell lines
Ruan, Ban-Feng,Wang, Si-Qi,Ge, Xiao-Lin,Yao, Ri-Sheng
, p. 2 - 9 (2014/01/06)
A new series of resveratrol acrylamides amine derivatives was designed, synthesized, and evaluated for their anti-proliferative activity against three cancer cell lines including human chronic myelocytic leukemia cell K562, human hepatoma HuH-7 and human lung carcinoma A549. Most of the compounds showed superior activity against three cell lines when compared to parent resveratrol. C13 had the best anti-tumor activity against the HuH-7 cell line and its IC 50 was 4.5 μmol/L; C16 had the best anti-tumor activity against the K562 cell line and its IC50 was 2.9 μmol/L; C18 had the best anti-tumor activity against the A549 cell line and its IC50 was 3.8 μmol/L. It could be seen that the activity of the aromatic amine derivatives was better than the fatty amine derivatives by analyzing the experimental data.
Development and SAR of functionally selective allosteric modulators of GABAA receptors
Alhambra, Cristobal,Becker, Chris,Blake, Timothy,Chang, Amy,Damewood Jr., James R.,Daniels, Thalia,Dembofsky, Bruce T.,Gurley, David A.,Hall, James E.,Herzog, Keith J.,Horchler, Carey L.,Ohnmacht, Cyrus J.,Schmiesing, Richard Jon,Dudley, Adam,Ribadeneira, Maria D.,Knappenberger, Katherine S.,MacIag, Carla,Stein, Mark M.,Chopra, Maninder,Liu, Xiaodong F.,Christian, Edward P.,Arriza, Jeffrey L.,Chapdelaine, Marc J.
experimental part, p. 2927 - 2938 (2011/06/21)
Positive modulators at the benzodiazepine site of α2- and α3-containing GABAA receptors are believed to be anxiolytic. Through oocyte voltage clamp studies, we have discovered two series of compounds that are positive modulators at α2-/α3-containing GABAA receptors and that show no functional activity at α1-containing GABA A receptors. We report studies to improve this functional selectivity and ultimately deliver clinical candidates. The functional SAR of cinnolines and quinolines that are positive allosteric modulators of the α2- and α3-containing GABAA receptors, while simultaneously neutral antagonists at α1-containing GABAA receptors, is described. Such functionally selective modulators of GABAA receptors are expected to be useful in the treatment of anxiety and other psychiatric illnesses.
