69935-12-2Relevant articles and documents
Peptide-Boronic Acid Inhibitors of Flaviviral Proteases: Medicinal Chemistry and Structural Biology
Nitsche, Christoph,Zhang, Linlin,Weigel, Lena F.,Schilz, Jonas,Graf, Dominik,Bartenschlager, Ralf,Hilgenfeld, Rolf,Klein, Christian D.
, p. 511 - 516 (2017/04/27)
A thousand-fold affinity gain is achieved by introduction of a C-terminal boronic acid moiety into dipeptidic inhibitors of the Zika, West Nile, and dengue virus proteases. The resulting compounds have Ki values in the two-digit nanomolar range
Synthesis and anti-tumor activity evaluation of Matijin-Su derivatives
Xu, Bixue,Wang, Ning,Pan, Weidong,Qiu, Jingying,Cao, Peixue,Zhu, Meifen,Feng, Yibin,Liang, Guangyi
, p. 34 - 40 (2014/06/24)
A series of Matijin-Su (MTS, N-(N-benzoyl-l-phenylalanyl)-O-acetyl-l- phenylalanol) derivatives was synthesized and evaluated for their anti-tumor activities in hepatocellular carcinoma cells. The IC50 of compounds 1, 3, 4, 11, 13 were less than 20 μM, and compound 1 and 3 showed an IC 50 value of less than 9 μM. Expansion inhibition could be found significantly in compound 1 and 3-treated human hepatoma cell HepG2 and PLC/PRF/5, while both compounds exhibit lower toxicity to human hepatocyte cell line L-02. Compound 1 and 3 could induce cell cycle arrest at G1/S phase. This may be attributed to increase level of intracellular reactive oxygen species (ROS). Up-regulation of p38 MAPK activity in responding the ROS stabilize p53 and activate p21 transcription, the critical regulatory in G1/S checkpoint. Observations in this study shed light on the potential of MTS derivatives compound 1 and 3 as novel suppressors to human liver cancer.
UNUSUAL AMINO ACIDS. III. ASYMMETRIC SYNTHESIS OF 3-ARYLALANINES
Taudien, Stefan,Schinkowski, Klaus,Krause, Hans-Walter
, p. 73 - 84 (2007/10/02)
21 (Z)-α-N-benzoylamino-β-arylacrylic acids and their esters were prepared by known procedures and hydrogenated to the corresponding optically active α-benzoyl-β-arylalanine derivatives with optical yields in the range of 82-95percent ee using the cationi