139243-55-3Relevant articles and documents
Stabilization of β-peptide helices by direct attachment of trifluoromethyl groups to peptide backbones
Cho, Joonil,Sawaki, Kyohei,Hanashima, Shinya,Yamaguchi, Yoshiki,Shiro, Motoo,Saigo, Kazuhiko,Ishida, Yasuhiro
, p. 9855 - 9858 (2014)
The 14-helix structure of oligo-β-peptides was significantly stabilized by direct attachment of CF3 groups to their backbones. Our studies indicate that this stabilization originates from the CF 3-promoted increase in the intramolecular hydrogen-bonding ability of their backbone amides, leading to a novel strategy to stabilize peptide folding.
An extension of the 'Bip method': Induced axial chirality in a series of dipeptides based on Bip/β2,2-HBip combined with Ala/β3-HAla
Dutot, Laurence,Gaucher, Anne,Wright, Karen,Wakselman, Michel,Mazaleyrat, Jean-Paul,Oancea, Simona,Peggion, Cristina,Formaggio, Fernando,Toniolo, Claudio
, p. 363 - 371 (2006)
In the search for an extension of the 'Bip method' for determining the absolute configuration of β-amino acids and β-peptides, dipeptides based on β2,2-HBip/l(d)-Ala, Bip/l-β3-HAla, and β2,2-HBip/l-β3-HAla were synthesized in solution and the induced circular dichroism (ICD) in their biphenyl core evaluated in comparison with the previously investigated Bip/l(d)-Ala series. Weak, poorly informative ICDs were observed in MeOH solution for the linear N-Boc protected dipeptide methyl esters based on β2,2-HBip, as well as for those with Ala/β3-HAla at the N-terminus of Bip/β2,2- HBip. However, a significant ICD was recorded for Boc-Bip-l-β3- HAla-OMe. These results were confirmed by low-temperature 1H NMR spectroscopy studies of the dipeptides in CDCl3 and CD3OD solutions, showing two diastereoisomeric conformers in significantly different populations for Boc-Bip-l-β3-HAla-OMe in CD3OD. In general, ICDs were found to be weaker for dipeptides containing β-amino acids as compared to those of their α-amino acid counterparts.
Aryl imidazole derivative and application thereof
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Paragraph 0258-0261, (2021/06/23)
The invention relates to an aryl imidazole derivative and application thereof. The aryl imidazole derivative is a compound shown as a formula (I) in the description or pharmaceutically acceptable salt thereof. The invention also discloses application of the aryl imidazole derivative in preparation of drugs for treating cancers. The invention further discloses application of the aryl imidazole derivative in preparation of drugs for treating diseases caused by EGFR mutation.