16607-60-6Relevant articles and documents
Dual Nickel- And Photoredox-Catalyzed Reductive Cross-Coupling of Aryl Halides with Dichloromethane via a Radical Process
Xu, Tao,Xu, Wenhao,Zheng, Purui
supporting information, (2020/11/13)
The first catalytic strategy to harness a new chloromethane radical from dichloromethane under dual Ni/photoredox catalytic conditions has been developed. Compared with traditional two-electron reductive process associated with metallic reductants, this method via a single-electron approach can proceed under exceptionally mild conditions (visible light, ambient temperature, no strong base) and exhibits complementary reactivity patterns. It affords a broad scope of many functional groups, including alkenyl, which suffers cyclopropanation in previous routes. The diarylmethane-d2 compounds can be readily available with this transformation.
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.
Large-scale synthesis of novel sterically hindered acenaphthene-based α-diimine ligands and their application in coordination chemistry
Guo, Lihua,Kong, Wenyu,Xu, Yanjian,Yang, Yuliang,Ma, Rui,Cong, Li,Dai, Shengyu,Liu, Zhe
supporting information, p. 58 - 67 (2018/02/14)
An efficient method to synthesize novel highly sterically hindered acenaphthene-based α-diimine ligands bearing bulky diarylmethyl moiety was achieved by two-step reactions. These reactions could be carried out on a scale of 100 g with no chromatography involved. On the basis of this method, a series of novel highly sterically hindered acenaphthene-based α-diimine Pd(II) and Ni(II) complexes, imidazolium precursors and the corresponding NHCs-metal complexes were also successfully synthesized. These novel complexes can offer great potential for metal-catalyzed polymerizations and organic reactions.
