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Synthesis and biological studies of new piperidino-1,2,3-triazole hybrids with 3-aryl isoxazole side chains.
Murthy, Appala Venkata Ramana; Narendar, Vennu; Sampath Kumar, Nangunoori; Aparna, Pasula; Bhavani, Anagani Kanaka Durga; Solhi, Hélène; Le Guevel, Rémy; Roul, Julie; Gautier, Fabien; Juin, Philippe; Reddy, Chada Raji; Mosset, Paul; Levoin, Nicolas; Grée, René.
Afiliación
  • Murthy AVR; Chemveda Life Sciences India Pvt. Ltd., #B-11/1, IDA Uppal, Hyderabad-500039, Telangana, India; Jawaharlal Nehru Technological University Hyderabad, Kukatpally, Hyderabad-500 085, Telangana, India.
  • Narendar V; Chemveda Life Sciences India Pvt. Ltd., #B-11/1, IDA Uppal, Hyderabad-500039, Telangana, India.
  • Sampath Kumar N; Chemveda Life Sciences India Pvt. Ltd., #B-11/1, IDA Uppal, Hyderabad-500039, Telangana, India.
  • Aparna P; Jawaharlal Nehru Technological University Hyderabad, Kukatpally, Hyderabad-500 085, Telangana, India.
  • Bhavani AKD; Osmania University, Department of Chemistry, Hyderabad 500007, Telangana, India.
  • Solhi H; Univ Rennes, Plateform ImPACcell, BIOSIT, F-35000 Rennes, France.
  • Le Guevel R; Univ Rennes, Plateform ImPACcell, BIOSIT, F-35000 Rennes, France.
  • Roul J; UMR 892 INSERM/6299 CNRS/Université de Nantes, Team 8 "Cell Survival and Tumor Escape in Breast Cancer", Institut de Recherche Thérapeutique de l'Université de Nantes, 8 Quai Moncousu, BP 70721, 44007 Nantes Cedex 1, France; Institut de Cancérologie de l'Ouest, Centre de Lutte contre le Cancer René
  • Gautier F; UMR 892 INSERM/6299 CNRS/Université de Nantes, Team 8 "Cell Survival and Tumor Escape in Breast Cancer", Institut de Recherche Thérapeutique de l'Université de Nantes, 8 Quai Moncousu, BP 70721, 44007 Nantes Cedex 1, France; Institut de Cancérologie de l'Ouest, Centre de Lutte contre le Cancer René
  • Juin P; UMR 892 INSERM/6299 CNRS/Université de Nantes, Team 8 "Cell Survival and Tumor Escape in Breast Cancer", Institut de Recherche Thérapeutique de l'Université de Nantes, 8 Quai Moncousu, BP 70721, 44007 Nantes Cedex 1, France.
  • Reddy CR; Department of Organic Synthesis & Process Chemistry, CSIR-Indian Institute of Chemical Technology, Hyderabad 500007, India.
  • Mosset P; Univ Rennes, CNRS, ISCR (Institut des Sciences Chimiques de Rennes), UMR 6226, F-35000 Rennes, France.
  • Levoin N; Bioprojet-Biotech, 4 rue du Chesnay Beauregard, BP 96205, 35762 Saint Grégoire, France.
  • Grée R; Univ Rennes, CNRS, ISCR (Institut des Sciences Chimiques de Rennes), UMR 6226, F-35000 Rennes, France.
Bioorg Med Chem Lett ; 52: 128390, 2021 11 15.
Article en En | MEDLINE | ID: mdl-34601029
A small library of new piperidine-triazole hybrids with 3-aryl isoxazole side chains has been designed and synthesized. Their cytotoxicity against a panel of seven cancer cell lines has been established. For the most promising compound, an IC50 value of 3.8 µM on PUMA/Bcl-xL interaction in live cancer cells was established through BRET analysis. A rationale was proposed for these results through complete molecular modelling studies.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Piperidinas / Triazoles / Isoxazoles / Antineoplásicos Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2021 Tipo del documento: Article País de afiliación: India Pais de publicación: Reino Unido

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Piperidinas / Triazoles / Isoxazoles / Antineoplásicos Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2021 Tipo del documento: Article País de afiliación: India Pais de publicación: Reino Unido