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- W2322143219 abstract "c-Met has emerged as an attractive target for targeted cancer therapy because of its abnormal activation in many cancer cells. To identify high potent and selective c-Met inhibitors, we started with profiling the potency and in vitro metabolic stability of a reported hit 7. By rational design, a novel sulfonylpyrazolo[4,3-b]pyridine 9 with improved DMPK properties was discovered. Further elaboration of π–π stacking interactions and solvent accessible polar moieties led to a series of highly potent and selective type I c-Met inhibitors. On the basis of in vitro and in vivo pharmacological and pharmacokinetics studies, compound 46 was selected as a preclinical candidate for further anticancer drug development." @default.
- W2322143219 created "2016-06-24" @default.
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- W2322143219 date "2015-02-25" @default.
- W2322143219 modified "2023-10-17" @default.
- W2322143219 title "Design and Optimization of a Series of 1-Sulfonylpyrazolo[4,3-<i>b</i>]pyridines as Selective c-Met Inhibitors" @default.
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- W2322143219 doi "https://doi.org/10.1021/jm502018y" @default.
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