Discovery of novel taspine derivatives as antiangiogenic agents

Jie Zhang; Yanmin Zhang; Sanqi Zhang; Sicen Wang; Langchong He

doi:10.1016/j.bmcl.2009.11.073

Discovery of novel taspine derivatives as antiangiogenic agents

Jie Zhang
, Yanmin Zhang
, Sanqi Zhang
, Sicen Wang
, Langchong He

Health Science Center

Xi'an Jiaotong University

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

36 Scopus citations

Abstract

VEGFR-2 plays a critical role in vasculogenesis and inhibitors of VEGFR-2 could be used in the treatment of cancer. Taspine was one of the active ingredients screened by using an endothelial cell membrane chromatography and showed inhibition against VEGFR-2. In our research, we explored how the lactone ring and biphenyl scaffold in taspine influence its potent in vitro anticancer and antiangiogenesis activities. Accordingly, we report the design, synthesis, and preliminary evaluation of four novel taspine derivatives as VEGFR-2 inhibitors. The preliminary biological test showed that one of the compounds showed much better inhibitory activities against CACO-2 (IC₅₀ = 52.5 nM) and ECV304 (IC₅₀ = 2.67 nM) than taspine. This result enlarges the interest in ring-opened taspine derivative skeleton in the search of new antiangiogenesis agents.

Original language	English
Pages (from-to)	718-721
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	20
Issue number	2
DOIs	https://doi.org/10.1016/j.bmcl.2009.11.073
State	Published - 15 Jan 2010

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

Antiangiogenesis
Taspine derivatives
Tyrosine kinase
VEGFR-2 Inhibitors

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10.1016/j.bmcl.2009.11.073

Cite this

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title = "Discovery of novel taspine derivatives as antiangiogenic agents",

abstract = "VEGFR-2 plays a critical role in vasculogenesis and inhibitors of VEGFR-2 could be used in the treatment of cancer. Taspine was one of the active ingredients screened by using an endothelial cell membrane chromatography and showed inhibition against VEGFR-2. In our research, we explored how the lactone ring and biphenyl scaffold in taspine influence its potent in vitro anticancer and antiangiogenesis activities. Accordingly, we report the design, synthesis, and preliminary evaluation of four novel taspine derivatives as VEGFR-2 inhibitors. The preliminary biological test showed that one of the compounds showed much better inhibitory activities against CACO-2 (IC50 = 52.5 nM) and ECV304 (IC50 = 2.67 nM) than taspine. This result enlarges the interest in ring-opened taspine derivative skeleton in the search of new antiangiogenesis agents.",

keywords = "Antiangiogenesis, Taspine derivatives, Tyrosine kinase, VEGFR-2 Inhibitors",

author = "Jie Zhang and Yanmin Zhang and Sanqi Zhang and Sicen Wang and Langchong He",

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TY - JOUR

T1 - Discovery of novel taspine derivatives as antiangiogenic agents

AU - Zhang, Jie

AU - Zhang, Yanmin

AU - Zhang, Sanqi

AU - Wang, Sicen

AU - He, Langchong

PY - 2010/1/15

Y1 - 2010/1/15

N2 - VEGFR-2 plays a critical role in vasculogenesis and inhibitors of VEGFR-2 could be used in the treatment of cancer. Taspine was one of the active ingredients screened by using an endothelial cell membrane chromatography and showed inhibition against VEGFR-2. In our research, we explored how the lactone ring and biphenyl scaffold in taspine influence its potent in vitro anticancer and antiangiogenesis activities. Accordingly, we report the design, synthesis, and preliminary evaluation of four novel taspine derivatives as VEGFR-2 inhibitors. The preliminary biological test showed that one of the compounds showed much better inhibitory activities against CACO-2 (IC50 = 52.5 nM) and ECV304 (IC50 = 2.67 nM) than taspine. This result enlarges the interest in ring-opened taspine derivative skeleton in the search of new antiangiogenesis agents.

AB - VEGFR-2 plays a critical role in vasculogenesis and inhibitors of VEGFR-2 could be used in the treatment of cancer. Taspine was one of the active ingredients screened by using an endothelial cell membrane chromatography and showed inhibition against VEGFR-2. In our research, we explored how the lactone ring and biphenyl scaffold in taspine influence its potent in vitro anticancer and antiangiogenesis activities. Accordingly, we report the design, synthesis, and preliminary evaluation of four novel taspine derivatives as VEGFR-2 inhibitors. The preliminary biological test showed that one of the compounds showed much better inhibitory activities against CACO-2 (IC50 = 52.5 nM) and ECV304 (IC50 = 2.67 nM) than taspine. This result enlarges the interest in ring-opened taspine derivative skeleton in the search of new antiangiogenesis agents.

KW - Antiangiogenesis

KW - Taspine derivatives

KW - Tyrosine kinase

KW - VEGFR-2 Inhibitors

UR - https://www.scopus.com/pages/publications/72549112083

U2 - 10.1016/j.bmcl.2009.11.073

DO - 10.1016/j.bmcl.2009.11.073

M3 - 文章

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AN - SCOPUS:72549112083

SN - 0960-894X

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SP - 718

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JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 2

ER -

Discovery of novel taspine derivatives as antiangiogenic agents

Abstract

UN SDGs

Keywords

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