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

• Main Authors: Xabier del Corte (Author), Adrián López-Francés (Author), Ilia Villate-Beitia (Author), Myriam Sainz-Ramos (Author), Edorta Martínez de Marigorta (Author), Francisco Palacios (Author), Concepción Alonso (Author), Jesús M. de los Santos (Author), José Luis Pedraz (Author), Javier Vicario (Author)
• Format: Book
• Published: MDPI AG, 2022-04-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

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...