No abstract

HUNI 068 is a promising new compound with activity even against MDR tumor cells. Further investigations into the class of ferrocene-derived agents might reveal compounds with improved activity for a more specific and safe anti-cancer therapy.

As a contribution to bioorganometallic chemistry, a dia‐ and enantioselective synthesis of novel carbocyclic amino acid analogues with a 1,2‐ferroceno‐fused cyclopentene backbone has been developed. Using two related planar‐chiral intermediates, i.e. (1S,E)‐ethyl‐3‐[2‐(phenylsulfonylacetyl)ferrocen‐1‐yl]acrylate, (1S,E)‐ethyl‐3‐[2‐(methoxycarbonyl)ferrocen‐1‐yl]acrylate, stereoselective entries to different tBoc‐ or Fmoc‐protected ferroceno‐fused 1‐amino‐3‐carboxyalkyl‐2‐cyclopentenes were elaborated. These compounds were then used for the preparation of metal‐containing peptides by means of solid‐phase peptide synthesis (SPPS). (© Wiley‐VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2009)

The conjugation of a ferrocenyl amino acid to the cell-penetrating peptide hCT(9-32) does not impair its ability to efficiently translocate into cells. Furthermore, the bioconjugate does not induce any cytotoxicity, thus presenting a potential electrochemical sensor suitable for the detection of living cells.