26867-13-0Relevant articles and documents
Synthesis and antiproliferative activity of some novel benzo-fused imidazo[1,8]naphthyridinones
Giannouli, Vassiliki,Kostakis, Ioannis K.,Pouli, Nicole,Marakos, Panagiotis,Samara, Pinelopi,Tsitsilonis, Ourania
, p. 2621 - 2623 (2015)
A number of new substituted fused naphthyridinones has been prepared and their antiproliferative activity was evaluated against a panel of seven human tumor cell lines, including the variant MES-SA/Dx5, reported to be 100-fold resistant to doxorubicin. Ce
Design and synthesis of diarylamines and diarylethers as cytotoxic antitumor agents
Wang, Xiao-Feng,Tian, Xing-Tao,Ohkoshi, Emika,Qin, Bingjie,Liu, Yi-Nan,Wu, Pei-Chi,Hour, Mann-Jen,Hung, Hsin-Yi,Qian, Keduo,Huang, Rong,Bastow, Kenneth F.,Janzen, William P.,Jin, Jian,Morris-Natschke, Susan L.,Lee, Kuo-Hsiung,Xie, Lan
supporting information, p. 6224 - 6228 (2012/10/29)
Based on a shared structural core of diarylamine in several known anticancer drugs as well as a new cytotoxic hit 6-chloro-2-(4-cyanophenyl)amino- 3-nitropyridine (7), 30 diarylamines and diarylethers were designed, synthesized, and evaluated for cytotoxic activity against A549, KB, KB-vin, and DU145 human tumor cell lines (HTCL). Four new leads 11e, 12, 13a, and 13b were discovered with GI50 values ranging from 0.33 to 3.45 μM. Preliminary SAR results revealed that a diarylamine or diarylether could serve as an active structural core, meta-chloro and ortho-nitro groups on the A-ring (either pyridine or phenyl ring) were necessary and crucial for cytotoxic activity, and the para-substituents on the other phenyl ring (B-ring) were related to inhibitory selectivity for different tumor cells. In an investigation of potential biological targets of the new leads, high thoughput kinase screening discovered that new leads 11e, 12 and 13b especially inhibit Mer tyrosine kinase, a proto-oncogene associated with munerous tumor types, with IC50 values of 2.2-3.0 μM. Therefore, these findings provide a good starting point to optimize a new class of compounds as potential anticancer agents, particularly targeting Mer tyrosine kinase.
PYRIDYL CARBENE PHOSPHORESCENT EMITTERS
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Page/Page column 73-74, (2012/09/22)
Organometallic compounds comprising an imidazole carbene ligand having a N- containing ring fused to the imidazole ring are provided. In particular, the N-containing ring fused to the imidazole ring may contain one nitrogen atom or more than one nitrogen