期刊
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
卷 2009, 期 16, 页码 2675-2686出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/ejoc.200900118
关键词
Azure B; Amination; Phenothiazine dye; Cell-penetrating peptide; Dye-peptide conjugate; Electronic spectra; Photodynamic therapy
资金
- Canadian Natural Sciences and Engineering Research Council (NSERC)
- QLT, Inc.
A high-yielding approach towards N-(2-aminoethyl)-Azure B has been established and extended towards the preparation of a functionalized peptide-dye synthetic precursor; Boc-protected 3-(alkylamino)phenothiazin-5-ium TFA. This has been utilized in a series of reactions with various amines towards nine novel 3,7-disubstituted phenothiazin-5-ium derivatives. Cleavage of the Boc group in the 3,7-disubstituted salts allowed a further seven novel dyes to be prepared and these have been utilized in a practical methodology designed for the synthesis of 13 novel phenothiazine-peptide conjugates. These peptide-photosensitizer vectors consist of a covalent attachment of a tethered dye to various protected amino acid moieties including the cell-penetrating peptide (CPP) octa-arginine and exhibit intense absorption maxima in the 623650 nm regions of the visible spectrum. The main goal of the studies is the design of cell-compatible photosensitisers that may be employed in photodynamic therapy. ((C) Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2009)
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