Discovery of novel bis-evodiamine derivatives with potent antitumor activity

Huixin Liang; Wei Wang; Fugui Zhu; Shuqiang Chen; Dan Liu; Chunquan Sheng

doi:10.1016/j.bmc.2022.116793

Discovery of novel bis-evodiamine derivatives with potent antitumor activity

Huixin Liang, Wei Wang, Fugui Zhu, Shuqiang Chen, Dan Liu, Chunquan Sheng

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

6 Scopus citations

Abstract

Inspired by antitumor natural product evodiamine, a series of novel bis-evodiamine derivatives were designed and synthesized, which showed potent antitumor activity. In particular, compound 13b effectively inhibited the proliferation and migration of HCT116 cells. Further mechanism studies revealed that compound 13b acted by inducing HCT116 cell apoptosis and arresting the cell cycle at the G2/M phase. Thus, compound 13b represents a promising lead compound for the discovery of novel antitumor agents.

Original language	English (US)
Article number	116793
Journal	Bioorganic and Medicinal Chemistry
Volume	65
DOIs	https://doi.org/10.1016/j.bmc.2022.116793
State	Published - Jul 1 2022
Externally published	Yes

Keywords

Antitumor activity
Apoptosis
Bis-evodiamine
Twin drug

ASJC Scopus subject areas

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

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10.1016/j.bmc.2022.116793

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title = "Discovery of novel bis-evodiamine derivatives with potent antitumor activity",

abstract = "Inspired by antitumor natural product evodiamine, a series of novel bis-evodiamine derivatives were designed and synthesized, which showed potent antitumor activity. In particular, compound 13b effectively inhibited the proliferation and migration of HCT116 cells. Further mechanism studies revealed that compound 13b acted by inducing HCT116 cell apoptosis and arresting the cell cycle at the G2/M phase. Thus, compound 13b represents a promising lead compound for the discovery of novel antitumor agents.",

keywords = "Antitumor activity, Apoptosis, Bis-evodiamine, Twin drug",

author = "Huixin Liang and Wei Wang and Fugui Zhu and Shuqiang Chen and Dan Liu and Chunquan Sheng",

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year = "2022",

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day = "1",

doi = "10.1016/j.bmc.2022.116793",

language = "English (US)",

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journal = "Bioorganic and Medicinal Chemistry",

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TY - JOUR

T1 - Discovery of novel bis-evodiamine derivatives with potent antitumor activity

AU - Liang, Huixin

AU - Wang, Wei

AU - Zhu, Fugui

AU - Chen, Shuqiang

AU - Liu, Dan

AU - Sheng, Chunquan

PY - 2022/7/1

Y1 - 2022/7/1

N2 - Inspired by antitumor natural product evodiamine, a series of novel bis-evodiamine derivatives were designed and synthesized, which showed potent antitumor activity. In particular, compound 13b effectively inhibited the proliferation and migration of HCT116 cells. Further mechanism studies revealed that compound 13b acted by inducing HCT116 cell apoptosis and arresting the cell cycle at the G2/M phase. Thus, compound 13b represents a promising lead compound for the discovery of novel antitumor agents.

AB - Inspired by antitumor natural product evodiamine, a series of novel bis-evodiamine derivatives were designed and synthesized, which showed potent antitumor activity. In particular, compound 13b effectively inhibited the proliferation and migration of HCT116 cells. Further mechanism studies revealed that compound 13b acted by inducing HCT116 cell apoptosis and arresting the cell cycle at the G2/M phase. Thus, compound 13b represents a promising lead compound for the discovery of novel antitumor agents.

KW - Antitumor activity

KW - Apoptosis

KW - Bis-evodiamine

KW - Twin drug

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DO - 10.1016/j.bmc.2022.116793

M3 - Article

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AN - SCOPUS:85129742469

SN - 0968-0896

VL - 65

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

M1 - 116793

ER -

Discovery of novel bis-evodiamine derivatives with potent antitumor activity

Abstract

Keywords

ASJC Scopus subject areas

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