Updated research and applications of small molecule inhibitors of Keap1-Nrf2 protein-protein interaction: a review

C Zhuang, Z Miao, C Sheng… - Current medicinal …, 2014 - ingentaconnect.com
The Keap1-Nrf2-ARE pathway is one of the most important regulators of cytoprotective
responses to oxidative and/or electrophilic stresses, which is believed to play a critical role …

Design and synthesis of new bioisosteres of spirooxindoles (MI-63/219) as anti-breast cancer agents

A Kumar, G Gupta, AK Bishnoi, R Saxena… - Bioorganic & Medicinal …, 2015 - Elsevier
We report herein the design and synthesis of bioisosteres of spirooxindole (MI-63/219), a
small-molecule inhibitors of the MDM2–p53 interaction as anti-breast cancer agents …

Design, synthesis and biological evaluation of novel 5-(4-chlorophenyl)-4-phenyl-4H-1, 2, 4-triazole-3-thiols as an anticancer agent

KR Patel, JG Brahmbhatt, PA Pandya, DG Daraji… - Journal of Molecular …, 2021 - Elsevier
Cellular tumor antigen p53 is significant for cancer prevention and its mutation is most
documented genomic change in human cancers. Thus, restoration of p53 function by …

Novel inhibitors of the MDM2-p53 interaction featuring hydrogen bond acceptors as carboxylic acid isosteres

AZ Gonzalez, Z Li, HP Beck, J Canon… - Journal of Medicinal …, 2014 - ACS Publications
We previously reported the discovery of potent and selective morpholinone and
piperidinone inhibitors of the MDM2-p53 interaction. These inhibitors have in common a …

[HTML][HTML] A multicomponent protocol for the synthesis of highly functionalized γ-lactam derivatives and their applications as antiproliferative agents

X Del Corte, A López-Francés, A Maestro… - Pharmaceuticals, 2021 - mdpi.com
An efficient synthetic methodology for the preparation of 3-amino 1, 5-dihydro-2 H-pyrrol-2-
ones through a multicomponent reaction of amines, aldehydes, and pyruvate derivatives is …

[HTML][HTML] Multicomponent synthesis of unsaturated γ-lactam derivatives. Applications as antiproliferative agents through the bioisosterism approach: Carbonyl vs …

X Del Corte, A López-Francés, I Villate-Beitia… - Pharmaceuticals, 2022 - mdpi.com
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 …

Synthesis and evaluation of spiroisoxazoline oxindoles as anticancer agents

CJA Ribeiro, JD Amaral, CMP Rodrigues… - Bioorganic & medicinal …, 2014 - Elsevier
Restoring p53 levels through disruption of p53–MDM2 interaction has been proved to be a
valuable approach in fighting cancer. We herein report the synthesis and evaluation of …

[HTML][HTML] Regio-and stereoselective synthesis of new spirooxindoles via 1, 3-dipolar cycloaddition reaction: Anticancer and molecular docking studies

G Lotfy, H El Sayed, MM Said, YMA Aziz… - … of Photochemistry and …, 2018 - Elsevier
Owing to their structural novelty and inherent three-dimensionality, spiro scaffolds have
been shown indisputable promise as chemopreventive agents. A new series of heterocycles …

Brönsted-Acid-Catalyzed Asymmetric Three-Component Reaction of Amines, Aldehydes, and Pyruvate Derivatives. Enantioselective Synthesis of Highly …

X Del Corte, A Maestro, J Vicario… - Organic …, 2018 - ACS Publications
Chiral phosphoric acids are efficient organocatalysts for the asymmetric three-component
reaction of amines, aldehydes, and pyruvate derivatives. Simultaneous condensation of …

[HTML][HTML] Recent synthetic approaches towards small molecule reactivators of p53

JL Silva, CGS Lima, LP Rangel, GDS Ferretti, FP Pauli… - Biomolecules, 2020 - mdpi.com
The tumor suppressor protein p53 is often called “the genome guardian” and controls the
cell cycle and the integrity of DNA, as well as other important cellular functions. Its main …