1099693-56-7Relevant articles and documents
Terphenyl-Based Small-Molecule Inhibitors of Programmed Cell Death-1/Programmed Death-Ligand 1 Protein-Protein Interaction
Muszak, Damian,Surmiak, Ewa,Plewka, Jacek,Magiera-Mularz, Katarzyna,Kocik-Krol, Justyna,Musielak, Bogdan,Sala, Dominik,Kitel, Radoslaw,Stec, Malgorzata,Weglarczyk, Kazimierz,Siedlar, Maciej,D?mling, Alexander,Skalniak, Lukasz,Holak, Tad A.
, p. 11614 - 11636 (2021/08/20)
We describe a new class of potent PD-L1/PD-1 inhibitors based on a terphenyl scaffold that is derived from the rigidified biphenyl-inspired structure. Using in silico docking, we designed and then experimentally demonstrated the effectiveness of the terphenyl-based scaffolds in inhibiting PD-1/PD-L1 complex formation using various biophysical and biochemical techniques. We also present a high-resolution structure of the complex of PD-L1 with one of our most potent inhibitors to identify key PD-L1/inhibitor interactions at the molecular level. In addition, we show the efficacy of our most potent inhibitors in activating the antitumor response using primary human immune cells from healthy donors.
C-H bond functionalization via hydride transfer: synthesis of dihydrobenzopyrans from ortho-vinylaryl akyl ethers
McQuaid, Kevin M.,Long, Jonathan Z.,Sames, Dalibor
supporting information; experimental part, p. 2972 - 2975 (2009/12/05)
The hydride transfer initiated cyclization ("HT-cyclization") of aryl alkyl ethers, which leads to direct coupling of sp3 C-H bonds and activated alkenes, is reported. Readily available salicylaldehyde derived ethers are converted in one step to dihydrobenzopyrans, an important class of heteroarenes frequently found in biologically active compounds. This process has not been previously reported, in contrast to known HTcyclizations of the corresponding fert-amines ("tert-amino effect" reactions).
