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- Title
Palladium(II)-Catalyzed Site-Selective C(sp<sup>3</sup>)−H Alkynylation of Oligopeptides: A Linchpin Approach for Oligopeptide-Drug Conjugation.
- Authors
Liu, Tao; Qiao, Jennifer X.; Poss, Michael A.; Yu, Jin ‐ Quan
- Abstract
The palladium(II)-catalyzed C(sp3)−H alkynylation of oligopeptides was developed with tetrabutylammonium acetate as a key additive. Through molecular design, the acetylene motif served as a linchpin to introduce a broad range of carbonyl-containing pharmacophores onto oligopeptides, thus providing a chemical tool for the synthesis and modification of novel oligopeptide-pharmacophore conjugates by C−H functionalization. Dipeptide conjugates with coprostanol and estradiol were synthesized by this method for potential application in targeted drug delivery to tumor cells with overexpressed nuclear hormone receptors.
- Subjects
PALLADIUM catalysts; OLIGOPEPTIDES; BIOCONJUGATES; ACETYLENE; NUCLEAR receptors (Biochemistry); PEPTIDES
- Publication
Angewandte Chemie, 2017, Vol 129, Issue 36, p11064
- ISSN
0044-8249
- Publication type
Article
- DOI
10.1002/ange.201706367