Design, synthesis and biological evaluation of novel pyrrolidone-based derivatives as potent p53-MDM2 inhibitors

Si, Dongjuan; Luo, Huijuan; Zhang, Xiaomeng; Yang, Kundi; Wen, Hongmei; Li, Wei; Liu, Jian

doi:10.1016/j.bioorg.2021.105268

Cited by 7 publications

(1 citation statement)

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“…Potent compound (15) (with IC 50 = 0.59 μM) tested against HCT116, which induces the activation of p53 and p21 proteins and causes cell cycle arrest in the G1/M phase and apoptosis. [79] Ramharter et al carried out a Davis-Beirut reaction of three components to obtain a potent MDM2-p53 inhibitor (16) (Figure 12). [80] Lama et al reported two compounds 17 (MMRi62) and 18 (MMRi67) as an MDM4-degrader and an enzymatic inhibitor of the MDM2-MDM4 E3 complex influences apoptosis in leukemia cells (Figure 13).…”

Section: Heterocycles As P53-mdm2 Interaction Inhibitorsmentioning

confidence: 99%

Insight on Heterocycles as p53‐MDM2 Protein‐Protein Interaction Inhibitors: Molecular Mechanism for p53 Activation

Basha,

Mohan

2024

ChemistrySelect

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Transcription factor p53, also known as tumor suppressor protein. Encoded by the TP53 gene, the guardian of genome p53 regulates many gene pathways. Nevertheless, the molecular mechanisms of p53 functioning have been known for a few decades, and the exact role of p53 in cancer therapy is unclear. Also, comprehensive literature on heterocycles as p53‐MDM2 protein‐protein interaction inhibitors is limited. This review covers the molecular mechanism for the p53‐MDM2 interaction and its inhibition by the heterocyclic small molecules. We hope the present comprehensive study will help to develop heterocycles as anticancer drugs that induce apoptosis in tumor cells.

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Section: Heterocycles As P53-mdm2 Interaction Inhibitorsmentioning

confidence: 99%