Optimization of 1-Methyl-3-(pyridin-3-yl)-1H-indol Derivatives as ROR1 Inhibitors with Improved Activity and Selectivity
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Q Zheng, X Qiu, D Luo, H Ma, Y Ming…
Journal of Medicinal …, 2025
ACS Publications
ROR1 has garnered significant attention as a therapeutic target in oncology due to its critical involvement in cancer malignancy. Several biologics targeting ROR1 have advanced to clinical trials, but the development of selective small-molecule inhibitors remains limited. In our previous work, we identified the indole-based LDR102 as a novel ROR1 inhibitor with promising antitumor efficacy. However, subsequent studies revealed its off-target activity against kinases such as c-Kit, AblT315I, and PDGFRαV561D, alongside suboptimal …
