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Development of 4′-Oxo-MLN4924 as potential neddylation inhibitors: Design, synthesis, anti-HCMV evaluation, and molecular docking

  • Kisu Sung
  • , Sehwan Oh
  • , Hong Rae Kim
  • , Seokhwan Hyeon
  • , Jin Hyun Ahn
  • , Suyeon Kim
  • , Vikas R. Aswar
  • , Sushil K. Tripathi
  • , Jinha Yu
  • , Lak Shin Jeong

Research output: Contribution to journalArticlepeer-review

1 Scopus citations

Abstract

MLN4924 (1), a neddylation inhibitor, has shown promising anticancer and antiviral properties. In this study, we designed and synthesized new derivatives of 4′-oxo-MLN4924, inspired by the structures of MLN4924 and another known neddylation inhibitor, referred to as compound 2. Like compound 2, we used a specific type of sugar molecule but incorporated a modified building block known as 7-deazapurine for the nucleobase part. Additionally, we arranged the sulfamate and 2′-hydroxyl as key functional groups. We found that the 2′-OH group is essential for activity against human cytomegalovirus (HCMV) using luciferase reporter assay. Molecular docking and molecular dynamics (MD) studies revealed that the conformation of the sugar moiety plays a crucial role in protein–ligand interactions. These studies suggest that derivatives with a bulky aromatic ring at the 6-position of the nucleobase are likely to have enhanced binding, which is supported by experimental findings.

Original languageEnglish
Article number101765
JournalResults in Chemistry
Volume11
DOIs
StatePublished - Oct 2024

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© 2024

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