Abstract
CK-571 is a recently developed smooth muscle and non-muscle (NM2) myosin specific compound inhibiting them with IC50 = 9 nM and 100 nM while cardiac and skeletal muscle myosins are inhibited with several magnitude weaker binding. CK-571 might have great medical potential in several diseases related to smooth muscle myosin and NM2 functions. We have synthesized several derivatives of CK-571 introducing structural modifications in its linker region. We tested these derivatives on skeletal, smooth, cardiac and NM2 A, B, C myosin isoforms. Our results may open novel perspectives in developing novel smooth and NM2 specific drug derivatives.
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