Fluorescent phosphoinositide 3-kinase inhibitors suitable for monitoring of intracellular distribution
The monitoring of the drug behavior and distribution in biological system can provide information whether drug reaches its desired target, and a biological rationale for the design of new therapeutics. We have developed a family of potent fluorescent PI3K
Kim, Donghee,Lee, Hyunseung,Jun, Hwiseok,Hong, Soon-Sun,Hong, Sungwoo
p. 2508 - 2516
(2011/06/17)
Development of new fluorescent xanthines as kinase inhibitors
"Chemical Equation Presented" An efficient and versatile synthetic approach for the preparation of highly substituted xanthine derivatives has been developed by a combination of direct N7- and C8-arylation. With this method, diverse xanthine analogues were prepared and potent kinase inhibitors could be identified. For example, compound 8a inhibits PI3Ks and proliferation in T47D tumor cells. In addition, these xanthine-based kinase inhibitors exhibited significant fluorescence emission in a concentration- dependent response.
Kim, Donghee,Jun, Hwiseok,Lee, Hyunseung,Hong, Soon-Sun,Hong, Sungwoo
supporting information; experimental part
p. 1212 - 1215
(2010/06/21)
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