HIF-1α inhibitors: Synthesis and biological evaluation of novel moracin O and P analogues

Yan Xia; Yinglan Jin; Navneet Kaur; Yongseok Choi; Kyeong Lee

doi:10.1016/j.ejmech.2011.03.022

HIF-1α inhibitors: Synthesis and biological evaluation of novel moracin O and P analogues

Yan Xia, Yinglan Jin, Navneet Kaur, Yongseok Choi, Kyeong Lee

Department of Biotechnology

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

52 Citations (Scopus)

Abstract

The natural products moracins O and P exhibited potent in vitro inhibitory activity against hypoxia-inducible factor (HIF-1), which is a key mediator during adaptation of cancer cells to tumour hypoxia. Systematic variations of the structures of benzofuran type moracins were made and structure-activity relationship analysis showed the importance of the 2-arylbenzofuran ring and the (R)-configuration of the core scaffold. Further evaluation of the representative compound 5 showed its inhibitory effect on HIF-1α protein accumulation and target gene expression under hypoxia.

Original language	English
Pages (from-to)	2386-2396
Number of pages	11
Journal	European Journal of Medicinal Chemistry
Volume	46
Issue number	6
DOIs	https://doi.org/10.1016/j.ejmech.2011.03.022
Publication status	Published - 2011 Jun

Keywords

Arylbenzofuran
HIF-1α
Moracin
Structure-activity relationships

ASJC Scopus subject areas

Pharmacology
Drug Discovery
Organic Chemistry

UN SDGs

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

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10.1016/j.ejmech.2011.03.022

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title = "HIF-1α inhibitors: Synthesis and biological evaluation of novel moracin O and P analogues",

abstract = "The natural products moracins O and P exhibited potent in vitro inhibitory activity against hypoxia-inducible factor (HIF-1), which is a key mediator during adaptation of cancer cells to tumour hypoxia. Systematic variations of the structures of benzofuran type moracins were made and structure-activity relationship analysis showed the importance of the 2-arylbenzofuran ring and the (R)-configuration of the core scaffold. Further evaluation of the representative compound 5 showed its inhibitory effect on HIF-1α protein accumulation and target gene expression under hypoxia.",

keywords = "Arylbenzofuran, HIF-1α, Moracin, Structure-activity relationships",

author = "Yan Xia and Yinglan Jin and Navneet Kaur and Yongseok Choi and Kyeong Lee",

note = "Funding Information: This study was supported by the National Research Foundation of Korea (NRF) grant (2010-0024391) and KRIBB/KRCF grant funded by the Korean Government . ",

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doi = "10.1016/j.ejmech.2011.03.022",

language = "English",

volume = "46",

pages = "2386--2396",

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TY - JOUR

T1 - HIF-1α inhibitors

T2 - Synthesis and biological evaluation of novel moracin O and P analogues

AU - Xia, Yan

AU - Jin, Yinglan

AU - Kaur, Navneet

AU - Choi, Yongseok

AU - Lee, Kyeong

N1 - Funding Information: This study was supported by the National Research Foundation of Korea (NRF) grant (2010-0024391) and KRIBB/KRCF grant funded by the Korean Government .

PY - 2011/6

Y1 - 2011/6

N2 - The natural products moracins O and P exhibited potent in vitro inhibitory activity against hypoxia-inducible factor (HIF-1), which is a key mediator during adaptation of cancer cells to tumour hypoxia. Systematic variations of the structures of benzofuran type moracins were made and structure-activity relationship analysis showed the importance of the 2-arylbenzofuran ring and the (R)-configuration of the core scaffold. Further evaluation of the representative compound 5 showed its inhibitory effect on HIF-1α protein accumulation and target gene expression under hypoxia.

AB - The natural products moracins O and P exhibited potent in vitro inhibitory activity against hypoxia-inducible factor (HIF-1), which is a key mediator during adaptation of cancer cells to tumour hypoxia. Systematic variations of the structures of benzofuran type moracins were made and structure-activity relationship analysis showed the importance of the 2-arylbenzofuran ring and the (R)-configuration of the core scaffold. Further evaluation of the representative compound 5 showed its inhibitory effect on HIF-1α protein accumulation and target gene expression under hypoxia.

KW - Arylbenzofuran

KW - HIF-1α

KW - Moracin

KW - Structure-activity relationships

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M3 - Article

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SN - 0223-5234

VL - 46

SP - 2386

EP - 2396

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

IS - 6

ER -

HIF-1α inhibitors: Synthesis and biological evaluation of novel moracin O and P analogues

Abstract

Keywords

ASJC Scopus subject areas

UN SDGs

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