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
Synthesis and Insecticidal Activity of Novel Nitropyridyl-Based Dichloropropene Ethers
Liu, Aiping,Yu, Wanqi,Liu, Minhua,Bai, Jianjun,Liu, Weidong,Liu, Xingping,Pei, Hui,Hu, Li,Huang, Mingzhi,Wang, Xiaoguang
, p. 7469 - 7475 (2015/09/15)
Dihalopropene ether insecticides are known for good features such as no cross-resistance to other insecticide classes and safety for mammals. Pyridalyl is the only currently commercialized dichloropropene ether insecticide; however, it contains a trifluoromethyl group, the synthesis of which requires harsh reagents and reaction conditions. To search for novel dihalopropene ethers with unique biological activities but without trifluoromethyl groups, a series of nitropyridyl-based dichloropropene ether analogues were synthesized by reacting nitro-based halopyridine with 2,6-dichloro-4-(3,3-dichloroallyloxy)phenol or 2,6-dichloro-4-(3,3-dichloroallyloxy)phenyl 3-hydroxypropyl ether. Bioassay showed that the compounds exhibited potent insecticidal activities against various lepidopteran pests. Particularly, 2,6-dichloro-4-(3,3-dichloroallyloxy)phenyl 3-(5-nitro-2-pyridyloxy)propyl ether (8e) was active against major agricultural pests, and its insecticidal potency was comparable to that of Pyridalyl. Besides the trifluoromethyl group in Pyridalyl, a nitro group on the 5-position of the pyridyl ring is also viable for the development of optimal insecticidal activity.
PYRIDYL CARBENE PHOSPHORESCENT EMITTERS
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, (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 a
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.
IMIDAZOPYRIDINE DERIVATIVES AS PI3K INHIBITORS
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Page/Page column 119, (2012/11/13)
New imidazopyridine derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Phosphoinositide 3-Kinases (PI3Ks).
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
2-(4-SUBSTITUTED PHENYLAMINO) POLYSUBSTITUTED PYRIDINE COMPOUNDS AS INHIBITORS OF NON-NUCLEOSIDE HIV REVERSE TRANSCRIPTASE, PREPARATION METHODS AND USES THEREOF
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Page/Page column 12, (2012/03/12)
The invention relates to 2-(4-Substituted phenylamino) polysubstituted pyridine compounds as inhibitors of non-nucleoside HIV reverse transcriptase, preparation methods and uses thereof. Specifically, the invention relates to compounds of formula I or the
Hit to lead evaluation of 1,2,3-triazolo[4,5-b]pyridines as PIM kinase inhibitors
Pastor, Joaquín,Oyarzabal, Julen,Saluste, Gustavo,Alvarez, Rosa María,Rivero, Virginia,Ramos, Francisco,Cendón, Elena,Blanco-Aparicio, Carmen,Ajenjo, Nuria,Cebriá, Antonio,Albarrán,Cebrián, David,Corrionero, Ana,Fominaya, Jesús,Montoya, Guillermo,Mazzorana, Marco
scheme or table, p. 1591 - 1597 (2012/04/10)
PIM kinases have become targets of interest due to their association with biochemical mechanisms affecting survival, proliferation and cytokine production. 1,2,3-Triazolo[4,5-b]pyridines were identified as PIM inhibitors applying a scaffold hopping approa
THE 2-(4-SUBSTITUTED PHENYLAMINO) POLYSUBSTITUTED PYRIDINE COMPOUNDS AS THE INHIBITORS OF NON-NUCLEOSIDE HIV REVERSE TRANSCRIPTASE, PRAPARATION METHODS AND USES THEREOF
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Page/Page column 16, (2011/08/08)
The invention relates to 2-(4-Substituted phenylamino) polysubstituted pyridine compounds as inhibitors of non-nucleoside HIV reverse transcriptase, preparation methods and uses thereof. Specifically, the invention relates to compounds of formula I or the
Synthesis and conformational properties of 2,6-bis-anilino-3-nitropyridines
Schmid, Sylvia,Roettgen, Martin,Thewalt, Ulf,Austel, Volkhard
, p. 3408 - 3421 (2007/10/03)
The synthesis of 2,6-bis-anilino-3-nitropyridines that are alkylated or acylated at the anilino nitrogen atoms is described. These derivatives show characteristic differences in the 1H-NMR spectra compared with the unsubstituted parent compound