Design, Synthesis and Antitumor Activity Evaluation of Novel Dual G9a/EZH2 Inhibitors.

Yajie Shi, Qiuyue Zhang, Maoying Zhang, Xiujuan Zhao, Shuhang Zhang, Jirui Li, Haofeng Li, Chenglin Fu, Guoliang Chen

Abstract read

In one paragraph

Article in Molecules (Basel, Switzerland), 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

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0citing papers in PubMed

–field-weighted citation impact

1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

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0 citing papers in PubMed.

No citing paper in PubMed yet.

4 · The record

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5 · Who and what money

Authors and funding

9 authors.

Yajie ShiCollege of Pharmacy, Heze University, Heze 274000, China.

Qiuyue ZhangDepartment of Pharmacology, Shenyang Pharmaceutical University, Shenyang 110016, China.

Maoying ZhangKey Laboratory of Structure-Based Drug Design & Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China.

Xiujuan ZhaoCollege of Pharmacy, Heze University, Heze 274000, China.

Shuhang ZhangCollege of Pharmacy, Heze University, Heze 274000, China.

Jirui LiCollege of Pharmacy, Heze University, Heze 274000, China.

Haofeng LiCollege of Pharmacy, Heze University, Heze 274000, China.

Chenglin FuCollege of Pharmacy, Heze University, Heze 274000, China.

Guoliang ChenKey Laboratory of Structure-Based Drug Design & Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Targeting the crosstalk between histone methyltransferases G9a and EZH2 represents a promising strategy for cancer therapy. To improve upon our previously reported dual inhibitor SU08, we rationally designed and synthesized five series (SU, UA, UB, N, and L) of novel G9a/EZH2 dual inhibitors, incorporating diverse pyridone, urea, and thienopyrimidine moieties, yielding a total of 43 compounds. In vitro enzymatic screening revealed that compound

Indexed as

Antineoplastic AgentsDrug DesignEnhancer of Zeste Homolog 2 ProteinEnzyme InhibitorsHistone-Lysine N-MethyltransferaseAnimalsCell Line, TumorCell ProliferationHistocompatibility AntigensHumansMiceMolecular Docking SimulationRatsStructure-Activity RelationshipAntineoplastic AgentsEHMT2 protein, humanEnhancer of Zeste Homolog 2 ProteinEnzyme InhibitorsHistocompatibility AntigensHistone-Lysine N-Methyltransferaseantitumordual-target inhibitorsEZH2G9a

Identifiers

PMID42883209

DOI10.3390/molecules31193446

PMCPMC13666074

What OpenQuestion holds

Textmetadata

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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.