Anti-cancer activity of novel dibenzo[b,f]azepine tethered isoxazoline derivatives

10.1186/1472-6769-12-5BMC Chemical Biology12

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N-(2-Chlorophenyl)-2-(1E)-(4-methoxyphenyl)-methyleneamino-4,5,6, 7-tetrahydro-1-benzo-thiophene-3-carboxamide

In the title compound, C24H24ClN2O 2S, the variations in the bond lengths and angles around the N atoms indicate delocalization of the N-atom lone pair. The molecular structure is stabilized by intramolecular N-H⋯N, N-H⋯Cl, C-H⋯S and C-H⋯O hydrogen bonds. © 2005 International Union of Crystallography Printed in Great Britain - all rights reserved

A one pot synthesis of novel bioactive tri- substitute-condensed-imidazopyridines that targets snake venom phospholipase A<inf>2</inf>

Drugs such as necopidem, saripidem, alpidem, zolpidem, and olprinone contain nitrogencontaining bicyclic, condensed-imidazo1,2-αpyridines as bioactive scaffolds. In this work, we report a high-yield one pot synthesis of 1-(2-methyl-8-aryl-substitued-imidazo1,2-α pyridin-3-yl)ethan-1-onefor the first-time. Subsequently, we performed in silico mode-ofaction analysis and predicted that the synthesized imidazopyridines targets Phospholipase A2 (PLA2). In vitro analysis confirmed the predicted target PLA2 for the novel imidazopyridine derivative1-(2-Methyl-8-naphthalen-1-yl-imidazo 1,2-αpyridine-3-yl)-ethanone (compound 3f) showing significant inhibitory activity towards snake venom PLA2 with an IC50 value of 14.3 μM. Evidently, the molecular docking analysis suggested that imidazopyridine compound was able to bind to the active site of the PLA2 with strong affinity, whose affinity values are comparable to nimesulide. Furthermore, we estimated the potential for oral bioavailability by Lipinski's Rule of Five. Hence, it is concluded that the compound 3f could be a lead molecule against snake venom PLA2. © 2015 Anilkumar et al.This is an open access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited

Breakup of the Neoarchean supercontinent Kenorland: Evidence from zircon and baddeleyite U-Pb ages of LIP-related mafic dykes in the Coorg Block, southern India

The Coorg Block in southern Peninsular India is one of the oldest crustal blocks on Earth that preserves the evidence for continental crust formation during the Paleo-Mesoarchean through subduction-related arc magmatism, followed by granulite facies metamorphism in the Mesoarchean. In this study, we report for the first time, the ‘bar codes’ of a major Paleoproterozoic Large Igneous Province in the Coorg Block through the finding of mafic dyke swarms. The gabbroic dykes from the Coorg Block, dominantly composed of plagioclase-pyroxene assemblage, show a restricted range in SiO2 values of 50.04–51.27 wt.%, and exhibit a sub-alkaline tholeiitic nature. These rocks show relatively flat LREE and constant HREE patterns and lack obvious Eu anomalies. Trace element modeling suggests that the dyke swarm was fed from a melt that originated at a shallow mantle level in the spinel stability field. Zircon grains are rare in the gabbro samples and those separated from two samples yielded 207Pb/206Pb weighted mean dates of 2214 ± 12 Ma and 2221 ± 7 Ma. The grains show magmatic features with depleted LREE and enriched HREE and positive Ce and negative Eu anomalies. Baddeleyite grains were dated from five gabbro samples which yielded 207Pb/206Pb weighted mean ages ranging between 2217 ± 7 Ma and 2228 ± 10 Ma. The combined data show a clear age peak at ca. 2.2 Ga. The mafic dykes in the Coorg Block show geochemical similarities with ca. 2.2 Ga mafic dyke swarms in different regions of the Dharwar and other cratons in Peninsular India and elsewhere on the globe. The data also support the inference that the global mafic magmatism at ca. 2.2 Ga was linked with intracontinental rifting of the Archean cratons through mantle upwelling or plume activity. We correlate the mafic dyke swarms in the Coorg Block with attempted rifting of the Neoarchean supercontinent Kenorland