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Anilinoquinazoline inhibitors of the RET kinase domain-elaboration of the 7-position.
Jordan, Allan M Begum, Habiba Fairweather, Emma E Fritzl, Samantha J R Goldberg, Kristin M Hopkins, Gemma V Hamilton, Niall M Lyons, Amanda J March, H Nikki Newton, Rebecca
Jordan, Allan M
Begum, Habiba
Fairweather, Emma E
Fritzl, Samantha J R
Goldberg, Kristin M
Hopkins, Gemma V
Hamilton, Niall M
Lyons, Amanda J
March, H Nikki
Newton, Rebecca
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Abstract
We have previously reported a series of anilinoquinazoline derivatives as potent and selective biochemical inhibitors of the RET kinase domain. However, these derivatives displayed diminished cellular potency. Herein we describe further optimisation of the series through modification of their physicochemical properties, delivering improvements in cell potency. However, whilst cellular selectivity against key targets could be maintained, combining cell potency and acceptable pharmacokinetics proved challenging.
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Date
2016-06-01
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Article
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Anilinoquinazoline inhibitors of the RET kinase domain-elaboration of the 7-position. 2016, 26 (11):2724-9 Bioorg Med Chem Lett