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• W2342013095 abstract "Our early structure–activity relationship study has identified benzo[b]carbazolone 6 as a high potency orally bioavailable ALK inhibitor. Further lead profiling disclosed that 6 is active against both ALK resistant and hot spot-activating mutants, and is also highly potent against RET kinase. Tumor stasis and partial tumor regression were achieved with 6 in both NIH/3T3-EML4-ALK and NIH/3T3-EML4-ALK L1196M xenograft models. Based on the optimal in vitro and in vivo antitumor efficacy, compound 6 is now being profiled further in our preclinical settings as a new orally available ALK/RET dual inhibitor." @default.
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• W2342013095 date "2016-08-01" @default.
• W2342013095 modified "2023-10-10" @default.
• W2342013095 title "An orally available tyrosine kinase ALK and RET dual inhibitor bearing the tetracyclic benzo[b]carbazolone core" @default.
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• W2342013095 doi "https://doi.org/10.1016/j.ejmech.2016.04.046" @default.
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