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- W2809849400 abstract "The abnormal expression of c-ros oncogene1 receptor tyrosine kinase (ROS1) has been identified as clinically actionable oncogenic driver in non-small-cell lung cancer. Since crizotinib was approved by the US FDA for the treatment of advanced ROS1-positive non-small-cell lung cancer, ROS1 kinase has become a promising therapeutic target. Under the guidance of some advanced computer-assisted technologies, such as structure-based drug design, homology modeling and lipophilic efficiency parameters, several potent and selective inhibitors against wild-type and mutant ROS1 were designed and synthesized. In this article, we will review a series of scaffolds targeting ROS1 kinase from the hit-to-drug evolution strategies of their representative compounds and it is hoped that these design strategies would facilitate medicinal chemists to optimize the process of drug design." @default.
- W2809849400 created "2018-07-10" @default.
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- W2809849400 date "2018-07-01" @default.
- W2809849400 modified "2023-09-25" @default.
- W2809849400 title "Evolution strategy of ROS1 kinase inhibitors for use in cancer therapy" @default.
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- W2809849400 doi "https://doi.org/10.4155/fmc-2018-0033" @default.
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