期刊论文Discovery and preclinical evaluations of TQB3616, a novel CDK4-biased inhibitor复制

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Z Xu, Y Liu, B Song, B Ren, X Xu, R Lin, X Zhu…
Bioorganic & Medicinal …, 2024
Elsevier
Abstract Among small-molecule CDK4/6 inhibitors (palbociclib, ribociclib, and abemaciclib) approved for metastatic breast cancers, abemaciclib has a more tolerable adverse effects in clinic. This is attributable to preferential inhibition of CDK4 over CDK6. In our search for a biased CDK4 inhibitor, we discovered a series of pyrimidine-indazole inhibitors. SAR studies led us to TQB3616 as a preferential CDK4 inhibitor. TQB3616 exhibited improvements in both enzymatic and cellular proliferation inhibitory potency when tested …