絞り込み

16641

広告

A general strategy for synthesis of cyclophane-braced peptide macrocycles via palladium-catalysed intramolecular spC-H arylation.

著者 Zhang X , Lu G , Sun M , Mahankali M , Ma Y , Zhang M , Hua W , Hu Y , Wang Q , Chen J , He G , Qi X , Shen W , Liu P , Chen G
Nat Chem.2018 Apr 02 ; ():.
この記事をPubMed上で見るPubMedで表示
この記事をGoogle翻訳上で見る Google翻訳で開く

スターを付ける スターを付ける     (3view , 0users)

Full Text Sources

Miscellaneous

New methods capable of effecting cyclization, and forming novel three-dimensional structures while maintaining favourable physicochemical properties are needed to facilitate the development of cyclic peptide-based drugs that can engage challenging biological targets, such as protein-protein interactions. Here, we report a highly efficient and generally applicable strategy for constructing new types of peptide macrocycles using palladium-catalysed intramolecular C(sp)-H arylation reactions. Easily accessible linear peptide precursors of simple and versatile design can be selectively cyclized at the side chains of either aromatic or modified non-aromatic amino acid units to form various cyclophane-braced peptide cycles. This strategy provides a powerful tool to address the long-standing challenge of size- and composition-dependence in peptide macrocyclization, and generates novel peptide macrocycles with uniquely buttressed backbones and distinct loop-type three-dimensional structures. Preliminary cell proliferation screening of the pilot library revealed a potent lead compound with selective cytotoxicity toward proliferative Myc-dependent cancer cell lines.
PMID: 29610465 [PubMed - as supplied by publisher]
印刷用ページを開く Endnote用テキストダウンロード