161510-66-3Relevant academic research and scientific papers
Design and synthesis of a novel class of furan-based molecules as potential 20S proteasome inhibitors
Fu, Yiqiu,Xu, Bo,Zou, Xiaomin,Ma, Chao,Yang, Xiaoming,Mou, Ke,Fu, Gang,Lue, Yang,Xu, Ping
, p. 1102 - 1106 (2007/10/03)
A novel class of furan-based compounds as potential 20S proteasome inhibitors have been designed and synthesized, among which nine compounds are peptide derivatives and six molecules are statine peptidomimetics. The C-terminal furanyl moiety was introduced to target molecules as furan-based amino acids. All the compounds were obtained steadily with moderate to high yield. Compound 12 was a selective moderate potent proteasome peptidomimetic inhibitor. It inhibited HepG2 and HL-60 proliferation effectively.
Structure-based optimisation of 2-aminobenzylstatine derivatives: Potent and selective inhibitors of the chymotrypsin-like activity of the human 20S proteasome
Furet, Pascal,Imbach, Patricia,Fuerst, Peter,Lang, Marc,Noorani, Maria,Zimmermann, Johann,Garcia-Echeverria, Carlos
, p. 1331 - 1334 (2007/10/03)
We have identified 2-aminobenzylstatine derivatives that inhibit non-covalently the chymotrypsin-like activity of the human 20S proteasome. A structure-based optimisation approach has allowed us to improve the potency of this structural class of proteasome inhibitors from micromolar to nanomolar level. The new derivatives showed good selectivity against the trypsin-like and post-glutamyl-peptide hydrolytic activities of this enzyme.
Inhibitors of HIV-1 proteinase containing 2-heterosubstituted 4-amino-3- hydroxy-5-phenylpentanoic acid: Synthesis, enzyme inhibition, and antiviral activity
Scholz,Billich,Charpiot,Ettmayer,Lehr,Rosenwirth,Schreiner,Gstach
, p. 3079 - 3089 (2007/10/02)
A convenient procedure for the synthesis of 2-heterosubstituted statine derivatives as novel building blocks in HIV-protease inhibitors has been developed. The synthesis starts with protected L-phenylalaninols, which were converted to γ-amino α,β-unsatura
