Synthesis and biological studies of new piperidino-1,2,3-triazole hybrids with 3-aryl isoxazole side chains.

Autor: 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 Gauducheau, Boulevard Jacques Monod, 44805 Saint Herblain-Nantes Cedex, France., 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 Gauducheau, Boulevard Jacques Monod, 44805 Saint Herblain-Nantes Cedex, France., 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.
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2021 Nov 15; Vol. 52, pp. 128390. Date of Electronic Publication: 2021 Sep 30.
DOI: 10.1016/j.bmcl.2021.128390
Abstrakt: 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 IC 50 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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Databáze: MEDLINE
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