Synthesis, biological and in silico evaluation of pure nucleobase-containing spiro (Indane-Isoxazolidine) derivatives as potential inhibitors of MDM2-p53 interaction

Maiuolo L. ; Algieri V. ; Russo B. ; Tallarida M.A. ; Nardi M. ; Gioia M.L.D. ; Merchant Z. ; Merino P. (Universidad de Zaragoza) ; Delso I. (Universidad de Zaragoza) ; Nino A.D.

Resumen: 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.

Idioma: Inglés

DOI: 10.3390/molecules24162909

Año: 2019

Publicado en: Molecules 24, 16 (2019), 2909 [14 pp.]
ISSN: 1420-3049

Factor impacto JCR: 3.267 (2019)

Categ. JCR: CHEMISTRY, MULTIDISCIPLINARY rank: 70 / 177 = 0.395 (2019) - Q2 - T2
Categ. JCR: BIOCHEMISTRY & MOLECULAR BIOLOGY rank: 141 / 297 = 0.475 (2019) - Q2 - T2

Factor impacto SCIMAGO: 0.698 - Pharmaceutical Science (Q1) - Chemistry (miscellaneous) (Q2) - Drug Discovery (Q2) - Physical and Theoretical Chemistry (Q2) - Organic Chemistry (Q2) - Analytical Chemistry (Q2) - Medicine (miscellaneous) (Q2) - Molecular Medicine (Q3)

Financiación: info:eu-repo/grantAgreement/ES/DGA/E34-R17
Financiación: info:eu-repo/grantAgreement/ES/MINECO/CTQ2016-76155-R

Tipo y forma: Artículo (Versión definitiva)

Área (Departamento): Área Química Orgánica (Dpto. Química Orgánica)