Abstract
AbstractThiazolium salts 2a–b derived from a dipeptide Boc‐Gly‐(Thz‐Ala)‐OMe (1b) containing the nonproteinogenic amino acid L‐thiazolylalanine (Thz‐Ala) can be used to generate the corresponding N,S‐heterocyclic carbene (NSHC) gold(I) (3a–b) and silver(I) (4) complexes. Reaction of the NSHC‐gold(I) iodide 3b with Boc‐Cys‐Gly‐OMe gives access to the peptide bioconjugate 5, which contains a NSHC‐Au‐(S‐Cys) unit. Compounds 3–5 constitute the first coin metal NSHC‐peptide complexes. All new compounds were comprehensively characterized by 1H, 13C and 2D‐NMR spectroscopy, IR spectroscopy, and mass spectrometry. Their cytotoxicity was studied in vitro against three different tumor cell lines (A549, Jurkat T and MiaPaca2) and IC50 values in the low micromolar range (< 25 μM), and as low as 0.4 μM in the best case were observed. All new Au complexes show good stability and promising properties and, as a result, this novel type of gold(I) carbene complex opens possibilities for the design of new metal‐based drugs with promising antitumor characteristics.
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