330550-92-0Relevant articles and documents
Design, synthesis and biological evaluation of novel pteridinone derivatives possessing a hydrazone moiety as potent PLK1 inhibitors
Hou, Yunlei,Hu, Tao,Li, Zhiwei,Liu, Yajing,Xu, Le,Yin, Bixi,Zhao, Yanfang,Zhu, Liangyu
, (2020)
A series of novel pteridinone derivatives possessing a hydrazone moiety were designed, synthesized and evaluated for their biological activity. Most of the synthesized compounds demonstrated moderate to excellent activity against A549, HCT116 and PC-3 cancer cell lines. In particular, compound L19 exhibited the most potent antiproliferative effects on three cell lines with IC50 values of 3.23 μM, 4.36 μM and 8.20 μM, respectively. In kinase assays, the compound L19 also showed potent inhibition activity toward PLK1 with % inhibition values of 75.1. Further mechanism studies revealed that compound L19 significantly inhibited proliferation of HCT-116 cell lines, induced a great decrease in mitochondrial membrane potential resulting in apoptosis of cancer cells, inhibited the migration of tumor cells, and arrested G1 phase of HCT116 cells.
Pteridinone compound and application thereof
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Paragraph 0020-0021, (2021/07/10)
The invention relates to a pteridinone compound. The chemical structure of the compound is shown as a formula (I). The pteridinone compound provided by the invention can inhibit cyclin dependent kinases (CDKs), especially CDK4 and CDK6, and has a remarkable effect of controlling proliferation of tumor cells of mammary gland, cervix uteri or colon, so that the compound can be used for preparing antitumor drugs.
The Discovery of 7-Methyl-2-[(7-methyl[1,2,4]triazolo[1,5- a]pyridin-6-yl)amino]-9-(tetrahydro-2 H-pyran-4-yl)-7,9-dihydro-8 H-purin-8-one (AZD7648), a Potent and Selective DNA-Dependent Protein Kinase (DNA-PK) Inhibitor
Goldberg, Frederick W.,Finlay, M. Raymond V.,Ting, Attilla K. T.,Beattie, David,Lamont, Gillian M.,Fallan, Charlene,Wrigley, Gail L.,Schimpl, Marianne,Howard, Martin R.,Williamson, Beth,Vazquez-Chantada, Mercedes,Barratt, Derek G.,Davies, Barry R.,Cadogan, Elaine B.,Ramos-Montoya, Antonio,Dean, Emma
supporting information, p. 3461 - 3471 (2020/02/04)
DNA-PK is a key component within the DNA damage response, as it is responsible for recognizing and repairing double-strand DNA breaks (DSBs) via non-homologous end joining. Historically it has been challenging to identify inhibitors of the DNA-PK catalyti