Evidence map›Paper›PMID 40928679›Full record

ArticleMolecular diversity2026

Design and synthesis of novel indolinone Aurora B kinase inhibitors based on fragment-based drug discovery (FBDD).

Baoxing Xie, Miaomiao Shi, Dan Tang, Shan Yang, Yan Zeng, Lifei Nie, Chao Niu

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Article in Molecular diversity, 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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4 · The record

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5 · Who and what money

Authors and funding

7 authors.

Baoxing XieState Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi, 830011, Xinjiang, China.
Miaomiao ShiState Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi, 830011, Xinjiang, China.
Dan TangState Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi, 830011, Xinjiang, China.
Shan YangState Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi, 830011, Xinjiang, China.
Yan ZengXinjiang Key Laboratory of Coal Mine Disaster Intelligent Prevention and Emergency Response, Xinjiang Institute of Engineering, Urumqi, 830023, China.
Lifei NieState Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi, 830011, Xinjiang, China.
Chao NiuState Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi, 830011, Xinjiang, China. niuchao@ms.xjb.ac.cn.

Funding

Natural Science Foundation of Xinjiang Uygur Autonomous Region 2022D01A339;2022D01A340Talent Project of Tianchi Young Doctoral Program in Xinjiang Uygur Autonomous 2024West Light Foundation, Chinese Academy of Sciences 2021-XBQNXZ-009West Light Foundation, Chinese Academy of Sciences 2023-XBQNXZ009
6 · The paper itself

Abstract

Aurora kinases are a group of serine/threonine kinases essential for cell mitosis, comprising Aurora A, B, and C. However, the Aurora B is overexpressed in multiple tumors and the aurone has been proved to exhibit potent inhibitory activity against Aurora B kinase by our group. The indolinone was considered as an aurone scaffold hopping analog, and the indolinone-based Aurora B inhibitor library (3577 molecules) was constructed by FBDD strategy. After pharmacophore model and molecular docking, the candidate molecules were identified, then synthesized via Suzuki-Miyaura and Knoevenagel reactions. The compounds 3-17a, 3-17d and 3-17 k especially inhibited Aurora B in the nanomolar range (IC

Indexed as

Antineoplastic AgentsAurora Kinase BDrug DesignDrug DiscoveryIndolesProtein Kinase InhibitorsCell Line, TumorCell ProliferationHumansMolecular Docking SimulationStructure-Activity RelationshipAntineoplastic AgentsAURKB protein, humanAurora Kinase BIndolesProtein Kinase InhibitorsAurora BFBDDIndolinone derivativesPharmacophoreTumor

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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.