116755-59-0Relevant articles and documents
Design and synthesis of Tr?ger's base ditopic receptors: host-guest interactions, a combined theoretical and experimental study
Bhaskar Reddy, Manda,Shailaja, Myadaraboina,Manjula, Alla,Premkumar, Joseph Richard,Sastry, Garikapati Narahari,Sirisha, Katukuri,Sarma, Akella Venkata Subrahmanya
, p. 1141 - 1149 (2015)
Two flexible Tr?ger's base ditopic receptors C4TB and C5TB incorporating monoaza crown ether were designed and synthesized for bisammonium ion complexation. A comprehensive study of host-guest interactions was established by 1H NMR spectroscopy
Design, synthesis, and biological study of 4-[(2-nitroimidazole-1h-alkyloxyl)aniline]-quinazolines as EGFR inhibitors exerting cytotoxicities both under normoxia and hypoxia
Cheng, Weiyan,Wang, Suhua,Yang, Zhiheng,Tian, Xin,Hu, Yongzhou
, p. 3079 - 3089 (2019)
Purpose: In order to get novel EGFR inhibitors exerting more potency in tumor hypoxia than in normoxia. Methods: A series of 4-[(2-nitroimidazole-1H-alkyloxyl)aniline]-quinazolines were designed and synthesized, and their in vitro cytotoxicity and EGFR inhibitory activity were evaluated. Molecule docking study was performed for the representative compound. Results: The structure-activity relationship (SAR) studies revealed that compounds bearing both meta-chloride and para-(2-nitroimidazole-1H-alkyloxy) groups on the aniline displayed potent inhibitory activities both in enzymatic and cellular levels. The most promising compound 16i potently inhibited EGFR with an IC50 value of 0.12 μM. Meanwhile, it manifested more potent cytotoxicity than the positive control lapatinib under tumor normoxia and hypoxia conditions (IC50 values of 1.59 and 1.09 μM against A549 cells, 2.46 and 1.35 μM against HT-29 cells, respectively). The proposed binding model of 16i in complex with EGFR was displayed by the docking results. Conclusion: This study provides insights for developing hypoxia-activated kinase inhibitors.
Synthesis of an 18F-labelled high affinity β1- adrenoceptor PET radioligand based on ICI 89,406
Wagner, Stefan,Law, Marilyn P.,Riemann, Burkhard,Pike, Victor W.,Breyholz, Hans-Joerg,Hoeltke, Garsten,Faust, Andreas,Renner, Christiane,Schober, Otmar,Schaefers, Michael,Kopka, Klaus
, p. 177 - 195 (2007/10/03)
To date, some non-selective β-adrenoceptor (β-AR) positron emission tomography (PET) radioligands are in clinical use, but no PET radioligand for the selective imaging of cardiac β1-ARs is clinically available. Therefore, the aim of this study
A multi-mode-driven molecular shuttle: Photochemically and thermally reactive azobenzene rotaxanes
Murakami, Hiroto,Kawabuchi, Atsushi,Matsumoto, Rika,Ido, Takeshi,Nakashima, Naotoshi
, p. 15891 - 15899 (2007/10/03)
The shuttling process of α-CyD in three rotaxanes (1-3) containing α-cyclodextrin (α-CyD) as a ring, azobenzene as a photoactive group, viologen as an energy barrier for slipping of the ring, and 2,4-dinitrobenzene as a stopper was investigated. The trans
1-[(Aryloxy)alkyl]-1H-imidazoles as inhibitors of neuronal nitric oxide synthase
Salerno,Sorrenti,Guerrera,Sarva,Siracusa,Di Giacomo,Vanella
, p. 491 - 494 (2007/10/03)
A series of 1-[(aryloxy)alkyl]-1 H-imidazoles were synthesized from imidazole and various (aryloxy)alkyl bromides and tested for inhibitory activity against the three isoforms of nitric oxide synthase. 1-[2-(4-Bromophenoxy)ethyl]-1 H-imidazole and 1-[2-[4-(trifluoromethyl)phenoxy]ethyl]-1H-imidazole showed inhibitory activity against the neuronal isoform but were less potent against the endothelial isoform. Thus they could be considered interesting for their selectivity. The remaining compounds had only modest activity.