cfi-400945 has been researched along with Breast-Neoplasms* in 1 studies
1 other study(ies) available for cfi-400945 and Breast-Neoplasms
Article | Year |
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Design, synthesis, and biological evaluation of novel pyrazolo [3,4-d]pyrimidine derivatives as potent PLK4 inhibitors for the treatment of TRIM37-amplified breast cancer.
Serine/threonine-protein kinase polo-like kinase 4 (PLK4) is a mitosis-associated protein kinase that plays a vital role in the duplication of centrioles in dividing cells and is considered a promising target of synthetic lethality in TRIM37-amplified breast cancer. Herein, based on a rational drug design strategy, we described a series of pyrazolo [3,4-d]pyrimidine derivatives as potent PLK4 inhibitors and dissected the relevant structure-activity relationships (SARs). Most compounds showed potent suppressive activities against PLK4, with IC Topics: Animals; Antineoplastic Agents; Breast Neoplasms; Cell Line, Tumor; Cell Proliferation; Drug Design; Drug Screening Assays, Antitumor; Female; Humans; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Pyrimidines; Rats; Rats, Sprague-Dawley; Structure-Activity Relationship; Tripartite Motif Proteins; Ubiquitin-Protein Ligases | 2022 |