6275-26-9Relevant articles and documents
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Loewenbein,Gagarin
, p. 2643 (1925)
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A Diarylacetonitrile as a Molecular Probe for the Detection of Polymeric Mechanoradicals in the Bulk State through a Radical Chain-Transfer Mechanism
Yamamoto, Takumi,Kato, Sota,Aoki, Daisuke,Otsuka, Hideyuki
, p. 2680 - 2683 (2021)
Since the beginning of polymer science, understanding the influence of mechanical stress on polymer chains has been a fundamental and important research topic. The detection of mechanoradicals generated by homolytic cleavage of the polymer chains in solut
Structure-based virtual screening, synthesis and biological evaluation of potential FAK-FAT domain inhibitors for treatment of metastatic cancer
Hiscox, Stephen E.,Jones, Samuel R.,Kandil, Sahar B.,Smith, Sonia,Westwell, Andrew D.
, (2020/08/28)
Focal adhesion kinase (FAK) is a tyrosine kinase that is overexpressed and activated in several advanced-stage solid cancers. In cancer cells, FAK promotes the progression and metastasis of tumours. In this study, we used structure-based virtual screening to filter a library of more than 210K compounds against the focal adhesion targeting FAK-focal adhesion targeting (FAT) domain to identify 25 virtual hit compounds which were screened in the invasive breast cancer line (MDA-MB-231). Most notably, compound I showed low micromolar antiproliferative activity, as well as antimigratory activity. Moreover, examination in a model of triple negative breast cancer (TNBC), revealed that, despite not effecting FAK phosphorylation, compound I significantly impairs proliferation whilst impairing focal adhesion growth and turnover leading to reduced migration. Further optimisation and synthesis of analogues of the lead compound I using a four-step synthetic procedure was performed, and analogues were assessed for their antiproliferative activity against three breast cancer (MDA-MB-231, T47D, BT474) cell lines and one pancreatic cancer (MIAPaCa2) cell line. Compound 5f was identified as a promising lead compound with IC50 values in the range of 4.59–5.28 μM in MDA-MB-231, T47D, BT474, and MIAPaCa2. Molecular modelling and pharmacokinetic studies provided more insight into the therapeutic features of this new series.
Switchable Stereoselectivity in Bromoaminocyclization of Olefins: Using Br?nsted Acids of Anionic Chiral Cobalt(III) Complexes
Jiang, Hua-Jie,Liu, Kun,Yu, Jie,Zhang, Ling,Gong, Liu-Zhu
supporting information, p. 11931 - 11935 (2017/09/20)
Br?nsted acids of anionic chiral CoIII complexes act as bifunctional phase-transfer catalysts to shuttle the substrates across the solvent interface and control stereoselectivity. The diastereomeric chiral CoIII-templated Br?nsted ac