TY - JOUR
T1 - Development of 4′-Oxo-MLN4924 as potential neddylation inhibitors
T2 - Design, synthesis, anti-HCMV evaluation, and molecular docking
AU - Sung, Kisu
AU - Oh, Sehwan
AU - Kim, Hong Rae
AU - Hyeon, Seokhwan
AU - Ahn, Jin Hyun
AU - Kim, Suyeon
AU - Aswar, Vikas R.
AU - Tripathi, Sushil K.
AU - Yu, Jinha
AU - Shin Jeong, Lak
N1 - Publisher Copyright:
© 2024
PY - 2024/10
Y1 - 2024/10
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=85203026985&partnerID=8YFLogxK
U2 - 10.1016/j.rechem.2024.101765
DO - 10.1016/j.rechem.2024.101765
M3 - Article
AN - SCOPUS:85203026985
SN - 2211-7156
VL - 11
JO - Results in Chemistry
JF - Results in Chemistry
M1 - 101765
ER -