86636-92-2Relevant academic research and scientific papers
Synthesis method of Acrylodan and analogues thereof
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, (2021/04/14)
The invention belongs to the technical field of synthesis of fluorescent probes in biochemistry, and particularly relates to an environment-sensitive fluorescent probe and a synthesis process route of Acrylodan and analogues thereof. A method comprises the following steps: taking 6-methoxy-2-acetyl naphthalene as a raw material, carrying out substitution reaction on the 6-methoxy-2-acetyl naphthalene and a lithium amide salt, carrying out addition elimination reaction on an obtained amino-substituted acetyl naphthalene product and trifluoroacetic acid, and then carrying out addition elimination reaction on the obtained amino-substituted acetyl naphthalene product and aldehydes to finally obtain the high-purity Acrylodan compound and analogues. The method has the advantages of simple synthesis steps, short reaction time, high yield, low production cost and the like, and solves the problems of complex synthesis steps, harsh synthesis conditions and expensive synthesis raw materials in original synthesis methods. The optimization and improvement of the synthetic process route of Acrylodan and analogues can greatly promote the application of the environment-sensitive probe in the field of biochemistry.
A Fluorescent Kinase Inhibitor that Exhibits Diagnostic Changes in Emission upon Binding
Fleming, Cassandra L.,Sandoz, Patrick A.,Inghardt, Tord,?nfelt, Bj?rn,Gr?tli, Morten,Andréasson, Joakim
supporting information, p. 15000 - 15004 (2019/09/17)
The development of a fluorescent LCK inhibitor that exhibits favourable solvatochromic properties upon binding the kinase is described. Fluorescent properties were realised through the inclusion of a prodan-derived fluorophore into the pharmacophore of an ATP-competitive kinase inhibitor. Fluorescence titration experiments demonstrate the solvatochromic properties of the inhibitor, in which dramatic increase in emission intensity and hypsochromic shift in emission maxima are clearly observed upon binding LCK. Microscopy experiments in cellular contexts together with flow cytometry show that the fluorescence intensity of the inhibitor correlates with the LCK concentration. Furthermore, multiphoton microscopy experiments demonstrate both the rapid cellular uptake of the inhibitor and that the two-photon cross section of the inhibitor is amenable for excitation at 700 nm.
