A QSAR study on inhibitory activities of 1-phenylbenzimidazoles against the platelet-derived growth factor receptor

Involvement of conformational isomerism in the complexity of the crystal network of 1-(4-nitrophenyl)-1H-1,3-benzimidazole derivatives driven by C—H...A (A = NO2, Npy and π) and orthogonal Npy...NO2 and ONO...Csp 2 interactions

“…It is worth mentioning the case of 1-(4-nitrophenyl)-1H-1,3benzimidazole, (I), which has been reported as an inhibitor of platelet-derived growth factor receptor (PDGFR), which is highly expressed in tumour cells (Zhong et al, 2004;Katritzky et al, 2005). Experimental evidence indicates that the inhibi-tory activity involves discrete noncovalent dipolar proteinligand interactions, which significantly contribute to the binding affinity and to intermolecular recognition.…”

Copper‐catalyzed N‐Arylation of Imidazoles with Aryl or Heteroaryl Halides Facilitated by Dimethylglyoxime in Water

“…[1][2][3][4] Although their synthesis has been accomplished successfully using aryllead triacetate, [5][6][7] triarylbismuth, 8 arylstannane, 9 arylsiloxanes 10 and arylboronic acid [11][12][13] reagents etc., these methods often employ expensive reagents or substrates requiring multistep syntheses, and some are highly toxic, which limits their utilization in synthetic chemistry.…”

π-stacking and C—X...D(X= H, NO2;D= O, π) interactions in the crystal network of both C—H...N and π-stacked dimers of 1,2-bis(4-bromophenyl)-1H-benzimidazole and 2-(4-bromophenyl)-1-(4-nitrophenyl)-1H-benzimidazole

“…Benzimidazoles with N-and C-bonded phenyl-ring substituents have been reported to have a wide range of pharmaceutical activities, such as acting as inhibitors of several growth factors (Katritzky et al, 2005;Smallheer et al, 2004;Zhong et al, 2004) and inhibitors of human cycloxygenases (Secci et al, 2012). Experimental evidence indicates that inhibitory activity involves discrete noncovalent dipolar protein-ligand interactions, which contribute significantly to binding affinity in molecular recognition.…”