Abstract:
:Some hybrid foldamers of various length, all containing the (4R,5S)-4-carboxy-5-methyloxazolidin-2-one (d-Oxd) moiety alternating with an l-amino acid (l-Val, l-Lys, or l-Ala), were prepared in order to study their preferred conformations and to evaluate their biological activity. Surprisingly, only the longer oligomers containing l-Ala fold into well-established helices, whereas all the other oligomers give partially unfolded turn structures. Nevertheless, they all show good biocompatibility, with no detrimental effects up to 64 μm. After equipping some selected foldamers with the fluorescent tag rhodamine B, a quantitative analysis was performed by dose- and time-response fluorescence-activated cell sorting (FACS) assays with human HeLa cells and primary blood lymphocytes, granulocytes, and monocytes. Among the cell types analyzed, the oligomers associated with monocytes and granulocytes with greatest efficacy, still visible after 24 h incubation. This effect is even more pronounced for foldamers that are able to form stable helices.
journal_name
ChemMedChemjournal_title
ChemMedChemauthors
Del Secco B,Malachin G,Milli L,Zanna N,Papini E,Cornia A,Tavano R,Tomasini Cdoi
10.1002/cmdc.201600597subject
Has Abstractpub_date
2017-02-20 00:00:00pages
337-345issue
4eissn
1860-7179issn
1860-7187journal_volume
12pub_type
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