4.7 Article

Fluorescent anticancer quinazolines as molecular probes for β-tubulin colchicine site competition assay and visualization of microtubules as intracellular targeting sites

Journal

DYES AND PIGMENTS
Volume 145, Issue -, Pages 233-238

Publisher

ELSEVIER SCI LTD
DOI: 10.1016/j.dyepig.2017.05.050

Keywords

Fluorescent probes; Fluorescence spectroscopy; UV/Vis spectroscopy; Inhibitors; Antiproliferation; Tubulin-binding agents

Funding

  1. Grant-in-Aid for Scientific Reseach (C) from the Japan Society for the Promotion of Science and Mext, Japan [15K07868]
  2. Region Basse Normandie (SEPEQ Project Asie 2015), France
  3. Grants-in-Aid for Scientific Research [15K07868] Funding Source: KAKEN

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Anticancer 2-aminoquinazolines were evaluated by their photophysical properties responding to media changes. By binding to the colchicine binding site of beta-tubulin, the fluorescence emission of 2-N-morpholino-derivative (1) was blue-shifted with enhanced intensity. These distinguished features were used for the development of a beta-tubulin colchicine site competition assay and visualization of the intracellular distribution of 1 by fluorescence microscopy.

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