85484-42-0Relevant articles and documents
Achieving cell penetration with distance-matching cysteine cross-linkers: A facile route to cell-permeable peptide dual inhibitors of Mdm2/Mdmx
Muppidi, Avinash,Wang, Zhiyong,Li, Xiaolong,Chen, Jiandong,Lin, Qing
, p. 9396 - 9398 (2011)
We report the design of bisarylmethylene bromides as a new class of rigid, distance-matching cysteine cross-linkers. By cross-linking a peptide dual inhibitor of Mdm2/Mdmx containing cysteines at i,i+7 positions, dramatic enhancement in cell permeability was achieved, along with increased helicity and biological activity.
Sequential one pot double C[sbnd]H heteroarylation of thiophene using bromopyridines to synthesize unsymmetrical 2,5-bipyridylthiophenes
Kieffer, Charline,Babin, Victor,Jouanne, Marie,Slimani, Ikram,Berhault, Yohann,Legay, Rémi,Sopková-de Oliveira Santos, Jana,Rault, Sylvain,Voisin-Chiret, Anne Sophie
, p. 5509 - 5516 (2017/08/22)
We present C[sbnd]H heteroarylation reactions between thiophene and variously substituted bromopyridines. The objective was to synthesize unsymmetrical 2,5-bipyridylthiophenes. We studied the reaction conditions allowing to a sequential one-pot double C[sbnd]H heteroarylation, in a view to introduce two different pyridyl moieties at positions 2 and 5 of the thiophene ring using bromopyridines. 11 original unsymmetrical 2,5-bipyridylthiophenes were synthesized and characterized, including 2,5-di(pyridin-2-yl)thiophenes for which the preparation by classical cross-coupling reactions is challenging. Finally, with the additional synthesis of both an unsymmetrical 2,5-biarylthiophene and an original pyrimidin-thiophene-furan scaffold, we shown that our methodology was also an efficient tool to access to new heterocyclic sequences.
Experimental and computational probes of a self-assembled capsule
Iwasawa, Tetsuo,Ajami, Dariush,Rebek Jr., Julius
, p. 2925 - 2928 (2007/10/03)
This research was undertaken to explore the interior surface of a synthetic receptor 1.1 with arylpyridines as guests. The interior surface differentiates the guests through the recognition of their nitrogen atoms. Experimental and computational analyses revealed that there is a delicate balance of attractions and repulsions between the host and the lone pairs of guests.