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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
Abstract : 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 : UV/Vis spectroscopy Inhibitors Fluorescence spectroscopy Tubulin-binding agents Fluorescent probes Antiproliferation
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https://hal-normandie-univ.archives-ouvertes.fr/hal-01844346
Contributor : Jocelyne Levillain <>
Submitted on : Thursday, July 19, 2018 - 11:54:19 AM
Last modification on : Thursday, July 2, 2020 - 3:21:37 AM

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COMUE-NORMANDIE | CNRS | ENSICAEN | UNICAEN | LCMT | UNILEHAVRE | INSA-ROUEN | UNIROUEN | INSA-GROUPE

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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, Elsevier, 2017, 145, pp.233-238. ⟨10.1016/j.dyepig.2017.05.050⟩. ⟨hal-01844346⟩

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