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^*

^*この論文の責任著者

和漢医薬学総合研究所研究開発部門資源開発分野（天然物創薬学領域）

研究成果: ジャーナルへの寄稿 › 学術論文 › 査読

114 被引用数 (Scopus)

抄録

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.

本文言語	英語
ページ（範囲）	5770-5773
ページ数	4
ジャーナル	Bioorganic and Medicinal Chemistry Letters
巻	21
号	19
DOI	https://doi.org/10.1016/j.bmcl.2011.08.005
出版ステータス	出版済み - 2011/10/01

ASJC Scopus 主題領域

生化学
分子医療
分子生物学
薬科学
創薬
臨床生化学
有機化学

UN SDG

この成果は、次の持続可能な開発目標に貢献しています

文献へのアクセス

10.1016/j.bmcl.2011.08.005

引用スタイル

@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",

volume = "21",

pages = "5770--5773",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier Ltd.",

number = "19",

}

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

抄録

ASJC Scopus 主題領域

UN SDG

文献へのアクセス

フィンガープリント

引用スタイル