Ma, Yuchi Sun, Guangqiang Chen, Danqi Peng, Xia Chen, Yue-Lei Su, Yi Ji, Yinchun Liang, Jin Wang, Xin Chen, Lin Ding, Jian Xiong, Bing Ai, Jing Geng, Meiyu Shen, Jingkang Design and Optimization of a Series of 1‑Sulfonyl­pyrazolo[4,3‑<i>b</i>]pyridines as Selective c‑Met Inhibitors 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 <b>7</b>. By rational design, a novel sulfonyl­pyrazolo­[4,3-<i>b</i>]­pyridine <b>9</b> 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 <b>46</b> was selected as a preclinical candidate for further anticancer drug development. series;DMPK properties;stability;type;sulfonyl;candidate;elaboration;moietie;Selective;cancer cells;pharmacokinetics studies;7.;activation;anticancer drug development;Optimization;potency;Series;basis;vivo;compound 46;interaction;Sulfonyl;inhibitor;cancer therapy 2015-03-12
    https://acs.figshare.com/articles/journal_contribution/Design_and_Optimization_of_a_Series_of_1_Sulfonyl_pyrazolo_4_3_i_b_i_pyridines_as_Selective_c_Met_Inhibitors/2186710
10.1021/jm502018y.s001