Development of pyrene-based fluorescent ether lipid as inhibitor of SK3 ion channels
نویسندگان
چکیده
We report the synthesis of three bioactive pyrene-based fluorescent analogues Ohmline which is most efficient and selective inhibitor SK3 ion channel. The interaction these Ohmline-pyrene (OP1-3) with liposomes different composition reveals that only OP2 OP3 are readily integrated into liposomes. Fluorescence measurements indicate that, depending on their concentration, exist either as monomer or a mixture excimers within liposome bilayer. Among Pyrene compounds able to reduce currents first modulator channel revealed by patch clamp (- 71.3 ± 13.3% at 10 μM) its inhibition SK3-dependent cancer cell migration (−32.5% 4.8% 1 μM). also fluorescence study living breast cells (MDA-MB-231) showing rapidly in bio-membranes followed internalization.
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ژورنال
عنوان ژورنال: European journal of medicinal chemistry
سال: 2021
ISSN: ['0009-4374']
DOI: https://doi.org/10.1016/j.ejmech.2020.112894