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Design, synthesis and structure-activity relationship study of novel indole-pyrrole scaffold compounds targeting Nur77 in colorectal tumor cells

delete2026-05-05
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PRE
AI
Q
Qi Zhao
J
Jingmei Liang
J
Jin Zhou
M
Meifeng Zeng
W
Wenbiao Zhang
Y
Yuan Cao
X
Xiaokun Zhang
X
Xiaohui Chen *
G
Guobin Xie *
Y
Ying Su *
Z
Zhiping Zeng *
DOI:10.1016/j.ejmech.2026.118927delete
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Abstract

Abstract

En 中文
• 1: New SIM-C-PhCF3+Cl- derivatives are rationally designed and synthesized. • 2: Compound A6 displays the most potent anti-proliferative activity against colorectal tumor cells. • 3: Compound A6 binds Nur77 with high affinity (Kd = 0.40 ± 0.05 μM). • 4: Compound A6 exhibits anti-mitotic activity in a Nur77-dependent manner. • 5: The SIM-C-PhCF3+Cl- are essential for the enhanced inhibitory effects on cell proliferation and mitotic arrest.
Keywords:
Nur77
colorectal tumor cells
anti-proliferative activity
mitotic arrest
structure-activity relationship

Journal

European Journal of Medicinal Chemistry cover
European Journal of Medicinal Chemistry
IF:
5.9
Papers:
1.7W
Citations:
6.0W

Organization

X
xiamen university
Scholars:
5.7W
Papers: 3.7W
Citations: 67
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