Multicomponent Synthesis of Unsaturated γ-Lactam Derivatives. Applications as Antiproliferative Agents through the Bioisosterism Approach: Carbonyl vs. Phosphoryl Group

We report efficient synthetic methodologies for the preparation of 3-amino and 3-hydroxy 3-pyrrolin-2-ones (unsaturated γ-lactams) through a multicomponent reaction of amines, aldehydes and acetylene or pyruvate derivatives. The densely substituted γ-lactam substrates show in vitro cytotoxicity, inh...

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Main Authors: Xabier del Corte, Adrián López-Francés, Ilia Villate-Beitia, Myriam Sainz-Ramos, Edorta Martínez de Marigorta, Francisco Palacios, Concepción Alonso, Jesús M. de los Santos, José Luis Pedraz, Javier Vicario
Format: Article
Language:English
Published: MDPI AG 2022-04-01
Series:Pharmaceuticals
Subjects:
Online Access:https://www.mdpi.com/1424-8247/15/5/511