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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 p-p 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. [ABSTRACT FROM AUTHOR]

We have developed a chromogenic and fluorescent chemodosimeter 3, based on a novel anion-catalyzed intramolecular hydrogen transfer, which displayed drastic changes in UV-Vis absorption as well as fluorescence emission intensities showing selectively for F− over other anions. [ABSTRACT FROM AUTHOR]