Design, synthesis, and biological evaluation of novel highly selective polo-like kinase 2 inhibitors based on the tetrahydropteridin chemical scaffold

MM Zhan, Y Yang, J Luo, XX Zhang, X Xiao, S Li… - European Journal of …, 2018 - Elsevier
Abstract Polo-like kinase 2 (Plk2) is a potential target for the treatment of cancer, which
displays an important role in tumor cell proliferation and survival. In this report, according to …

Structure-based design and SAR development of novel selective polo-like kinase 1 inhibitors having the tetrahydropteridin scaffold

X Lv, X Yang, MM Zhan, P Cao, S Zheng… - European Journal of …, 2019 - Elsevier
Abstract Polo-like kinase 1 (Plk1) is a validated target for the treatment of cancer. In this
report, by analyzing amino acid residue differences among the ATP-binding pockets of Plk1 …

[HTML][HTML] A selective inhibitor of the Polo-box domain of Polo-like kinase 1 identified by virtual screening

S Abdelfatah, A Berg, M Böckers, T Efferth - Journal of Advanced Research, 2019 - Elsevier
Abstract Polo-like kinase 1 (PLK1), a member of the Polo-like kinase family, plays an
important regulatory role in mitosis and cell cycle progression. PLK1 overexpression is …

Design, Synthesis, and Evaluation of Non‐ATP‐Competitive Small‐Molecule Polo‐Like Kinase 1 (Plk1) Inhibitors

DX Chen, J Huang, M Liu, YG Xu… - Archiv der …, 2015 - Wiley Online Library
A series of small‐molecule Plk1 inhibitors targeting the substrate‐binding pocket were
designed through rational drug design for the first time. The designed compounds were …

Design, synthesis, and biological evaluation of novel dihydropteridone derivatives possessing oxadiazoles moiety as potent inhibitors of PLK1

Z Li, S Mei, J Liu, J Huang, H Yue, T Ge, K Wang… - European Journal of …, 2023 - Elsevier
Abstract Polo like kinase 1 (PLK1) is a serine/threonine kinase that is widely distributed in
eukaryotic cells and plays an important role in multiple phases of the cell cycle. Its …

Discovery of Non‐ATP‐Competitive Inhibitors of Polo‐like Kinase 1

T Yun, T Qin, Y Liu, L Lai - ChemMedChem, 2016 - Wiley Online Library
Abstract Polo‐like kinase 1 (Plk1) is an evolutionarily conserved serine/threonine kinase,
and its N‐terminal kinase domain (KD) controls cell signaling through phosphorylation …

[HTML][HTML] MCC1019, a selective inhibitor of the Polo-box domain of Polo-like kinase 1 as novel, potent anticancer candidate

S Abdelfatah, A Berg, Q Huang, LJ Yang… - … Pharmaceutica Sinica B, 2019 - Elsevier
Abstract Polo-like kinase (PLK1) has been identified as a potential target for cancer
treatment. Although a number of small molecules have been investigated as PLK1 inhibitors …

Diversity evolution and jump of Polo-like kinase 1 inhibitors

C Liao, RS Yao - Science China Chemistry, 2013 - Springer
Abstract Polo-like kinase 1 (Plk1), a member of a family of serine/threonine kinases, is an
attractive target for the development of anticancer drugs because it is involved in the …

Identification of inhibitors of the polo-box domain of polo-like kinase 1 from natural and semisynthetic compounds

S Abdelfatah, E Fleischer, A Klinger, VKW Wong… - Investigational New …, 2020 - Springer
PLK1 has an important role in the regulation of cell cycle and represents an important target
for cancer treatment. This enzyme belongs to the Polo-like kinases family, which is …

5-(2-amino-pyrimidin-4-yl)-1H-pyrrole and 2-(2-amino-pyrimidin-4-yl)-1, 5, 6, 7-tetrahydro-pyrrolo [3, 2-c] pyridin-4-one derivatives as new classes of selective and …

M Caruso, B Valsasina, D Ballinari, J Bertrand… - Bioorganic & medicinal …, 2012 - Elsevier
The discovery and characterization of two new chemical classes of potent and selective Polo-
like kinase 1 (PLK1) inhibitors is reported. For the most interesting compounds, we discuss …