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

Yumiko Suzuki (1) , Jun-Ichi Sawada (2) , Paulina Hibner (3) , Hirosuke Ishii (2) , Kenji Matsuno (2) , Masayuki Sato (2) , Bernhard Witulski (3) , Akira Asai (2)

1 Sophia University [Tokyo]
2 University of Shizuoka
3 LCMT - Laboratoire de chimie moléculaire et thioorganique

Anticancer 2-aminoquinazolines were evaluated by their photophysical properties responding to media changes. By binding to the colchicine binding site of β-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 β-tubulin colchicine site competition assay and visualization of the intracellular distribution of 1 by fluorescence microscopy.

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

Domains: Chemical Sciences

Yumiko Suzuki, Jun-Ichi Sawada, Paulina Hibner, Hirosuke Ishii, Kenji Matsuno, et al.. Fluorescent anticancer quinazolines as molecular probes for ß-tubulin colchicine site competition assay and visualization of microtubules as intracellular targeting sites. Dyes and Pigments, 2017, 145, pp.233-238. ⟨10.1016/j.dyepig.2017.05.050⟩. ⟨hal-01844346⟩