Design and synthesis of indol-2-one derivatives as potential RET inhibitors

Zhenzhu Li; Kai Sun; Yuanhong Xu; Fuli Zhu; Zhenyu Mao; Yang Wang; Yaxia Yuan; Ting Qiu; Xiabin Chen; Lei Ma

doi:10.1016/j.bmcl.2023.129538

Design and synthesis of indol-2-one derivatives as potential RET inhibitors

Zhenzhu Li, Kai Sun, Yuanhong Xu, Fuli Zhu, Zhenyu Mao, Yang Wang, Yaxia Yuan, Ting Qiu, Xiabin Chen, Lei Ma

Department of Biochemistry & Structural Biology

Research output: Contribution to journal › Article › peer-review

Abstract

We synthesized and assessed five series of indol-2-one derivatives for their potential as RET kinase inhibitors. Notably, compounds B3, B6, D1, D2, D3, and D5 demonstrated significant inhibitory activity. Among these, D5 exhibited the best activity of inhibiting RET kinase, which provided reference for the subsequent development of RET kinase inhibitors as anti-thyroid cancer chemical.

Original language	English (US)
Article number	129538
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	97
DOIs	https://doi.org/10.1016/j.bmcl.2023.129538
State	Published - Dec 15 2023

Keywords

Cell proliferation
Indol-2-one
RET kinase inhibitors
Structure-activity relationship
Structure-based optimization

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/j.bmcl.2023.129538

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title = "Design and synthesis of indol-2-one derivatives as potential RET inhibitors",

abstract = "We synthesized and assessed five series of indol-2-one derivatives for their potential as RET kinase inhibitors. Notably, compounds B3, B6, D1, D2, D3, and D5 demonstrated significant inhibitory activity. Among these, D5 exhibited the best activity of inhibiting RET kinase, which provided reference for the subsequent development of RET kinase inhibitors as anti-thyroid cancer chemical.",

keywords = "Cell proliferation, Indol-2-one, RET kinase inhibitors, Structure-activity relationship, Structure-based optimization",

author = "Zhenzhu Li and Kai Sun and Yuanhong Xu and Fuli Zhu and Zhenyu Mao and Yang Wang and Yaxia Yuan and Ting Qiu and Xiabin Chen and Lei Ma",

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doi = "10.1016/j.bmcl.2023.129538",

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TY - JOUR

T1 - Design and synthesis of indol-2-one derivatives as potential RET inhibitors

AU - Li, Zhenzhu

AU - Sun, Kai

AU - Xu, Yuanhong

AU - Zhu, Fuli

AU - Mao, Zhenyu

AU - Wang, Yang

AU - Yuan, Yaxia

AU - Qiu, Ting

AU - Chen, Xiabin

AU - Ma, Lei

PY - 2023/12/15

Y1 - 2023/12/15

N2 - We synthesized and assessed five series of indol-2-one derivatives for their potential as RET kinase inhibitors. Notably, compounds B3, B6, D1, D2, D3, and D5 demonstrated significant inhibitory activity. Among these, D5 exhibited the best activity of inhibiting RET kinase, which provided reference for the subsequent development of RET kinase inhibitors as anti-thyroid cancer chemical.

AB - We synthesized and assessed five series of indol-2-one derivatives for their potential as RET kinase inhibitors. Notably, compounds B3, B6, D1, D2, D3, and D5 demonstrated significant inhibitory activity. Among these, D5 exhibited the best activity of inhibiting RET kinase, which provided reference for the subsequent development of RET kinase inhibitors as anti-thyroid cancer chemical.

KW - Cell proliferation

KW - Indol-2-one

KW - RET kinase inhibitors

KW - Structure-activity relationship

KW - Structure-based optimization

UR - http://www.scopus.com/inward/record.url?scp=85179685538&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=85179685538&partnerID=8YFLogxK

U2 - 10.1016/j.bmcl.2023.129538

DO - 10.1016/j.bmcl.2023.129538

M3 - Article

C2 - 39491121

AN - SCOPUS:85179685538

SN - 0960-894X

VL - 97

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

M1 - 129538

ER -

Design and synthesis of indol-2-one derivatives as potential RET inhibitors

Abstract

Keywords

ASJC Scopus subject areas

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