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Synthesis, Biological and In Silico Evaluation of Pure Nucleobase-Containing Spiro (Indane-Isoxazolidine) Derivatives as Potential Inhibitors of MDM2–p53 Interaction

Dipartimento di Chimica e Tecnologie Chimiche, Via P. Bucci, cubo 12C, Università della Calabria, 87036 Rende (CS), Italy
Dipartimento di Scienze della Salute, Università Magna Græcia, Viale Europa, Germaneto, 88100 Catanzaro, Italy
Dipartimento di Farmacia e Scienze della Salute e della Nutrizione, Edificio Polifunzionale, Università della Calabria, 87036 Rende (CS), Italy
Department of Pharmaceutics, UCL School of Pharmacy, London NW14NS, UK
Unidad de Glicobiología, Instituto de Biocomputación y Física de Sistemas Complejos (BIFI), Universidad de Zaragoza, 50009 Zaragoza, Spain
Departamento de Síntesis y Estructura de Biomoléculas, Instituto de Síntesis Química y Catálisis Homogénea (ISQCH), Universidad de Zaragoza-CSIC, 50009 Zaragoza, Spain
Authors to whom correspondence should be addressed.
Molecules 2019, 24(16), 2909;
Received: 9 July 2019 / Revised: 26 July 2019 / Accepted: 7 August 2019 / Published: 10 August 2019
(This article belongs to the Special Issue Computational Methods for Drug Discovery and Design)
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Nucleobase-containing isoxazolidines spiro-bonded to an indane core have been synthesized in very good yields by regio- and diastereoselective 1,3-dipolar cycloaddition starting from indanyl nitrones and N-vinylnucleobases by using environmentally benign microwave technology. The contemporary presence of various structural groups that are individually active scaffolds of different typology of drugs, has directed us to speculate that these compounds may act as inhibitors of MDM2–p53 interaction. Therefore, both computational calculations and antiproliferative screening against A549 human lung adenocarcinoma cells and human SH-SY5Y neuroblastoma cells were carried out to support this hypothesis. View Full-Text
Keywords: spirooxindoles; isoxazolidines; MDM2–p53 inhibition; indane derivatives spirooxindoles; isoxazolidines; MDM2–p53 inhibition; indane derivatives

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Maiuolo, L.; Algieri, V.; Russo, B.; Tallarida, M.A.; Nardi, M.; Di Gioia, M.L.; Merchant, Z.; Merino, P.; Delso, I.; De Nino, A. Synthesis, Biological and In Silico Evaluation of Pure Nucleobase-Containing Spiro (Indane-Isoxazolidine) Derivatives as Potential Inhibitors of MDM2–p53 Interaction. Molecules 2019, 24, 2909.

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