Pancreatic anticancer activity of a novel geranylgeranylated coumarin derivative

Tehsina Devji; Claire Reddy; Christina Woo; Suresh Awale; Shigetoshi Kadota; Dora Carrico-Moniz

doi:10.1016/j.bmcl.2011.08.005

Pancreatic anticancer activity of a novel geranylgeranylated coumarin derivative

Tehsina Devji, Claire Reddy, Christina Woo, Suresh Awale, Shigetoshi Kadota, Dora Carrico-Moniz^*

^*Corresponding author for this work

Section of Natural Products & Drug Discovery, Division of Medicinal Resources, Institute of Natural Medicine

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

114 Scopus citations

Abstract

A series of hydroxycoumarin derivatives has been synthesized and evaluated against human pancreatic PANC-1 cancer cells under nutrient-deprived conditions. Several compounds exhibited 100% preferential cytotoxicity at low micromolar concentrations under nutrition starvation, and showed no cytotoxicity under nutrient-rich conditions. In this study, a novel geranylgeranylated ether coumarin derivative 9 was found to exhibit the highest cytotoxic activity of 6.25 μM within 24 h. The preferential anti-tumor activity exhibited by compound 9 against PANC-1 under low oxygen and nutrient environment illustrates its great potential as a promising lead structure for the development of novel agents to combat pancreatic cancer.

Original language	English
Pages (from-to)	5770-5773
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	21
Issue number	19
DOIs	https://doi.org/10.1016/j.bmcl.2011.08.005
State	Published - 2011/10/01

Keywords

Anticancer agents
Coumarins
PANC-1
Pancreatic cancer
Preferential cytotoxicity

ASJC Scopus subject areas

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

UN SDGs

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

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10.1016/j.bmcl.2011.08.005

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@article{333f415dd287472cb5b4ef0c0d4c4bc0,

title = "Pancreatic anticancer activity of a novel geranylgeranylated coumarin derivative",

abstract = "A series of hydroxycoumarin derivatives has been synthesized and evaluated against human pancreatic PANC-1 cancer cells under nutrient-deprived conditions. Several compounds exhibited 100% preferential cytotoxicity at low micromolar concentrations under nutrition starvation, and showed no cytotoxicity under nutrient-rich conditions. In this study, a novel geranylgeranylated ether coumarin derivative 9 was found to exhibit the highest cytotoxic activity of 6.25 μM within 24 h. The preferential anti-tumor activity exhibited by compound 9 against PANC-1 under low oxygen and nutrient environment illustrates its great potential as a promising lead structure for the development of novel agents to combat pancreatic cancer.",

keywords = "Anticancer agents, Coumarins, PANC-1, Pancreatic cancer, Preferential cytotoxicity",

author = "Tehsina Devji and Claire Reddy and Christina Woo and Suresh Awale and Shigetoshi Kadota and Dora Carrico-Moniz",

note = "Funding Information: This work was supported in part by a faculty award grant from Wellesley College, MA. Biological studies were supported by a grant from the {\textquoteleft}Toyama Support Center for the Advanced Young Scientists in Life Sciences{\textquoteright}. The authors wish to thank Adina Badea and Myriam Taibi for their help with product isolation and compound characterization.",

year = "2011",

month = oct,

day = "1",

doi = "10.1016/j.bmcl.2011.08.005",

language = "英語",

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journal = "Bioorganic and Medicinal Chemistry Letters",

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TY - JOUR

T1 - Pancreatic anticancer activity of a novel geranylgeranylated coumarin derivative

AU - Devji, Tehsina

AU - Reddy, Claire

AU - Woo, Christina

AU - Awale, Suresh

AU - Kadota, Shigetoshi

AU - Carrico-Moniz, Dora

N1 - Funding Information: This work was supported in part by a faculty award grant from Wellesley College, MA. Biological studies were supported by a grant from the ‘Toyama Support Center for the Advanced Young Scientists in Life Sciences’. The authors wish to thank Adina Badea and Myriam Taibi for their help with product isolation and compound characterization.

PY - 2011/10/1

Y1 - 2011/10/1

N2 - A series of hydroxycoumarin derivatives has been synthesized and evaluated against human pancreatic PANC-1 cancer cells under nutrient-deprived conditions. Several compounds exhibited 100% preferential cytotoxicity at low micromolar concentrations under nutrition starvation, and showed no cytotoxicity under nutrient-rich conditions. In this study, a novel geranylgeranylated ether coumarin derivative 9 was found to exhibit the highest cytotoxic activity of 6.25 μM within 24 h. The preferential anti-tumor activity exhibited by compound 9 against PANC-1 under low oxygen and nutrient environment illustrates its great potential as a promising lead structure for the development of novel agents to combat pancreatic cancer.

AB - A series of hydroxycoumarin derivatives has been synthesized and evaluated against human pancreatic PANC-1 cancer cells under nutrient-deprived conditions. Several compounds exhibited 100% preferential cytotoxicity at low micromolar concentrations under nutrition starvation, and showed no cytotoxicity under nutrient-rich conditions. In this study, a novel geranylgeranylated ether coumarin derivative 9 was found to exhibit the highest cytotoxic activity of 6.25 μM within 24 h. The preferential anti-tumor activity exhibited by compound 9 against PANC-1 under low oxygen and nutrient environment illustrates its great potential as a promising lead structure for the development of novel agents to combat pancreatic cancer.

KW - Anticancer agents

KW - Coumarins

KW - PANC-1

KW - Pancreatic cancer

KW - Preferential cytotoxicity

UR - http://www.scopus.com/inward/record.url?scp=80052579118&partnerID=8YFLogxK

U2 - 10.1016/j.bmcl.2011.08.005

DO - 10.1016/j.bmcl.2011.08.005

M3 - 学術論文

C2 - 21880488

AN - SCOPUS:80052579118

SN - 0960-894X

VL - 21

SP - 5770

EP - 5773

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 19

ER -

Pancreatic anticancer activity of a novel geranylgeranylated coumarin derivative

Abstract

Keywords

ASJC Scopus subject areas

UN SDGs

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