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

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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