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Synthesis, crystal structure and effect of indeno[1,2-b]indole derivatives on prostate cancer in vitro. Potential effect against MMP-9.
Lobo, Gricela; Monasterios, Melina; Rodrigues, Juan; Gamboa, Neira; Capparelli, Mario V; Martínez-Cuevas, Javier; Lein, Michael; Jung, Klaus; Abramjuk, Claudia; Charris, Jaime.
Affiliation
  • Lobo G; Laboratorio de Síntesis Orgánica, Unidad de Bioquímica, Facultad de Farmacia, Universidad Central de Venezuela, Apartado 47206, Los Chaguaramos, 1041-A Caracas, Venezuela.
  • Monasterios M; Laboratorio de Síntesis Orgánica, Unidad de Bioquímica, Facultad de Farmacia, Universidad Central de Venezuela, Apartado 47206, Los Chaguaramos, 1041-A Caracas, Venezuela.
  • Rodrigues J; Laboratorio de Síntesis Orgánica, Unidad de Bioquímica, Facultad de Farmacia, Universidad Central de Venezuela, Apartado 47206, Los Chaguaramos, 1041-A Caracas, Venezuela.
  • Gamboa N; Laboratorio de Síntesis Orgánica, Unidad de Bioquímica, Facultad de Farmacia, Universidad Central de Venezuela, Apartado 47206, Los Chaguaramos, 1041-A Caracas, Venezuela.
  • Capparelli MV; Unidad de Estructura Molecular, Fundación Instituto de Estudios Avanzados (IDEA), Apartado 17606, Caracas 1015-A, Venezuela.
  • Martínez-Cuevas J; Servicio de Difracción de Rayos X, Universidad Autónoma de Barcelona, 08193 Barcelona, Spain.
  • Lein M; Department of Urology, University Hospital Charité, Campus Mitte, Schumannstrasse 20/21, 10117 Berlin, Germany; Berlin Institute for Urologic Research, Schumannstrasse 22/21, 10117 Berlin, Germany.
  • Jung K; Department of Urology, University Hospital Charité, Campus Mitte, Schumannstrasse 20/21, 10117 Berlin, Germany; Berlin Institute for Urologic Research, Schumannstrasse 22/21, 10117 Berlin, Germany.
  • Abramjuk C; Department of Urology, University Hospital Charité, Campus Mitte, Schumannstrasse 20/21, 10117 Berlin, Germany; Department of Experimental Medicine (FEM), University Hospital Charité, Campus Mitte, Charitéplatz 1, 10117 Berlin, Germany.
  • Charris J; Laboratorio de Síntesis Orgánica, Unidad de Bioquímica, Facultad de Farmacia, Universidad Central de Venezuela, Apartado 47206, Los Chaguaramos, 1041-A Caracas, Venezuela. Electronic address: jaime.charris@ucv.ve.
Eur J Med Chem ; 96: 281-95, 2015.
Article in En | MEDLINE | ID: mdl-25899333
A highly regiospecific synthesis of a series of indenoindoles is reported, together with X-ray studies and their activity against human prostate cancer cells PC-3 and LNCaP in vitro. The most effective compound 7,7-dimethyl-5-[(3,4-dichlorophenyl)]-(4bRS,9bRS)-dihydroxy-4b,5,6,7,8,9bhexahydro-indeno[1,2-b]indole-9,10-dione 7q reduced the viability in both cell lines in a time and dose-dependent manner. Inhibitory effects were also observed on the adhesion, migration, and invasion of the prostate cancer cells as well as on clonogenic possibly by inhibition of MMP-9 activity. Molecular docking of 7q and 6k into MMP-9 human active site was also performed to determine the probable binding mode.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Prostatic Neoplasms / Matrix Metalloproteinase 9 / Matrix Metalloproteinase Inhibitors / Indenes / Indoles / Antineoplastic Agents Limits: Humans / Male Language: En Journal: Eur J Med Chem Year: 2015 Document type: Article Affiliation country: Venezuela Country of publication: France
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Prostatic Neoplasms / Matrix Metalloproteinase 9 / Matrix Metalloproteinase Inhibitors / Indenes / Indoles / Antineoplastic Agents Limits: Humans / Male Language: En Journal: Eur J Med Chem Year: 2015 Document type: Article Affiliation country: Venezuela Country of publication: France