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Chen L.-T.,Tianjin Medical University | Chen H.,Tianjin Key Laboratory for Biomarkers of Occupational and Environmental Hazards | Zhou J.,Tianjin Medical University
Acta Crystallographica Section E: Structure Reports Online | Year: 2011

The title compound, C20H20N2O4, crystallizes with four independent molecules in the asymmetric unit. In the molecules, the dihedral angles between the benzene rings and indole mean planes are 24.5 (1), 22.5 (1), 8.8 (1) and 13.9 (1)°. In the crystal, intermolecular N -H⋯O hydrogen bonds are present between the imino groups and the adjacent carbonyl groups. π-π stacking is also observed with a centroidcentroid distance between nearly parallel pyrrole rings of 3.745 (3) Å.


Xu Z.-W.,Medical College | Wang F.-M.,Tianjin 3rd Central Hospital | Gao M.-J.,Medical College | Chen X.-Y.,Medical College | And 6 more authors.
Journal of Steroid Biochemistry and Molecular Biology | Year: 2011

Recent studies revealed the potential of Na+/K +-ATPase as a target for anticancer therapy and showed additional modes of action of cardiotonic steroids (CSs), a diverse family of naturally derived compounds, as inhibitors of Na+/K+-ATPase. The results from epidemiological studies showed significantly lower mortality rates in cancer patients receiving CSs, which sparked interest in the anticancer properties of these drugs. The present study was designed to investigate the anticancer effect of CSs (ouabain or cinobufagin) and to elucidate the molecular mechanisms of CS activity in hepatoma cell lines (HepG2 and SMMC-7721). Ouabain and cinobufagin significantly inhibited cell proliferation by attenuating the phosphorylation of extracellular regulated kinase (ERK) and down-regulating the expression of C-myc. These CSs also induced cell apoptosis by increasing the concentration of intracellular free calcium ([Ca2+]i) and induced S phase cell cycle arrest by down-regulating the expression of Cyclin A, cyclin dependent kinase 2 (CDK2) and proliferating cell nuclear antigen (PCNA) as well as up-regulating the expression of cyclin dependent kinase inhibitor 1A (p21CIP1). Overexpression of ERK reversed the antiproliferation effect of ouabain or cinobufagin in HepG2 and SMMC-7721 cells. Currently, the first generation of CS-based anticancer drugs (UNBS1450 and Anvirzel) are in Phase I clinical trials. These data clearly support their potential use as cancer therapies. © 2011 Elsevier Ltd. All rights reserved.


Tang X.-W.,Tianjin Medical University | Chen H.,Tianjin Key Laboratory for Biomarkers of Occupational and Environmental Hazards | Tian D.-L.,Tianjin Medical University | Shi S.-Y.,Tianjin Medical University
Acta Crystallographica Section E: Structure Reports Online | Year: 2011

In the title compound, C16H20N2O 3, the crystal packing is stabilized by weak π-π stacking interactions [centroid-centroid distances = 3.577 (9) and 3.693 (9) Å] and intermolecular C-H⋯O and N-H⋯O hydrogen-bond interactions. The C atoms of the N-isopropyl group are disordered over two sets of sites with occupancies of 0.61(3) and 0.39(3).


Tian D.-L.,Tianjin Medical University | Luo G.,Tianjin Medical University | Chen H.,Tianjin Key Laboratory for Biomarkers of Occupational and Environmental Hazards
Acta Crystallographica Section E: Structure Reports Online | Year: 2011

In title compound, C 16H 17FN 2O 2, the cyclo-hexane ring adopts a chair conformation. The crystal packing is stabilized by weak π-π stacking inter-actions [centroid-centroid distance = 3.503 (5) Å] and inter-molecular C - H⋯O, N - H⋯O and N - H⋯F hydrogen-bond inter-actions. © Tian et al. 2011.


Zhu T.-L.,Medical College | Jin J.-R.,General Unit | Chen H.,Tianjin Key Laboratory for Biomarkers of Occupational and Environmental Hazards | Chen H.,Medical College | And 2 more authors.
Acta Crystallographica Section E: Structure Reports Online | Year: 2011

In the title compound, C29H28ClNO7, the tetra-hydro-furan ring and the six-membered ring fused to it both display envelope conformations. The dihedral angles between the plane of the benzene ring of the benzo[d][1,3]dioxole system and the planes of the other two benzene rings are 80.59 (3) and 63.60 (2)°.

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