NDLI: A Multicomponent Protocol for the Synthesis of Highly Functionalized γ-Lactam Derivatives and Their Applications as Antiproliferative Agents

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A Multicomponent Protocol for the Synthesis of Highly Functionalized γ-Lactam Derivatives and Their Applications as Antiproliferative Agents

Content Provider	MDPI
Author	Adri, án López-Francés Corte, Xabier del Maestro, Aitor Villate-Beitia, Ilia Sainz-Ramos, Myriam de Marigorta, Edorta Martínez Pedraz, José Palacios, Francisco Vicario, Javier
Copyright Year	2021
Description	An efficient synthetic methodology for the preparation of 3-amino 1,5-dihydro-2H-pyrrol-2-ones through a multicomponent reaction of amines, aldehydes, and pyruvate derivatives is reported. In addition, the densely substituted lactam substrates show in vitro cytotoxicity, inhibiting the growth of carcinoma human tumor cell lines HEK293 (human embryonic kidney), MCF7 (human breast adenocarcinoma), HTB81 (human prostate carcinoma), HeLa (human epithelioid cervix carcinoma), RKO (human colon epithelial carcinoma), SKOV3 (human ovarian carcinoma), and A549 (carcinomic human alveolar basal epithelial cell). Given the possibilities in the diversity of the substituents that offer the multicomponent synthetic methodology, an extensive structure-activity profile is presented. In addition, both enantiomers of phosphonate-derived γ-lactam have been synthesized and isolated and a study of the cytotoxic activity of the racemic substrate vs. its two enantiomers is also presented. Cell morphology analysis and flow cytometry assays indicate that the main pathway by which our compounds induce cytotoxicity is based on the activation of the intracellular apoptotic mechanism.
Starting Page	782
e-ISSN	14248247
DOI	10.3390/ph14080782
Journal	Pharmaceuticals
Issue Number	8
Volume Number	14
Language	English
Publisher	MDPI
Publisher Date	2021-08-09
Access Restriction	Open
Subject Keyword	Pharmaceuticals Biochemistry and Molecular Biology Γ-lactams Multicomponent Synthesis Antiproliferative Effect
Content Type	Text
Resource Type	Article

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