62938-98-1Relevant academic research and scientific papers
Design and synthesis of potential β-sheet nucleators via Suzuki coupling reaction
Perissutti, Elisa,Frecentese, Francesco,Lavecchia, Antonio,Fiorino, Ferdinando,Severino, Beatrice,De Angelis, Francesca,Santagada, Vincenzo,Caliendo, Giuseppe
, p. 12779 - 12785 (2008/03/13)
Three series of compounds characterized by biphenylic structure were synthesized in order to develop new scaffolds able to induce β-sheet folding in the peptides. Microwave flash heating was used in order to shorten reaction times and to enhance the obtained yields. Simulated annealing molecular dynamics simulations demonstrated that some of the compounds were capable of adopting a 15-membered intramolecularly hydrogen-bonded conformation, which supports an antiparallel β-sheet structure.
Synthesis of substituted 5[H]phenanthridin-6-ones as potent poly(ADP-ribose)polymerase-1 (PARP1) inhibitors
Li, Jia-He,Serdyuk, Larisa,Ferraris, Dana V.,Xiao, Ge,Tays, Kevin L.,Kletzly, Paul W.,Li, Weixing,Lautar, Susan,Zhang, Jie,Kalish, Vincent J.
, p. 1687 - 1690 (2007/10/03)
1-, 2-, 3-, 4-, 8-, or 10-Substituted 5(H)phenanthridin-6-ones were synthesized and found to be potent PARP1 inhibitors. Among the 28 compounds prepared, some showed not only low IC50 values (compound 1b, 10 nM) but also desirable water solubility characteristics. These properties, which are superior to the common PARP1 inhibitors such as benzamides and isoquinolin-1-ones, are essential for potential therapeutic usage. The variety of compounds allows SAR analysis of favored substituents and substituted positions on 5(H)phenanthridin-6-one ring.
