2,6-Dithienyl-4-furyl pyridines: Synthesis, topoisomerase I and II inhibition, cytotoxicity, structure-activity relationship, and docking study

Arjun Basnet; Pritam Thapa; Radha Karki; Hoyoung Choi; Jae Hun Choi; Minho Yun; Byeong Seon Jeong; Yurngdong Jahng; Younghwa Na; Won Jea Cho; Youngjoo Kwon; Chong Soon Lee; Eung Seok Lee

doi:10.1016/j.bmcl.2009.11.041

2,6-Dithienyl-4-furyl pyridines: Synthesis, topoisomerase I and II inhibition, cytotoxicity, structure-activity relationship, and docking study

Arjun Basnet
, Pritam Thapa
, Radha Karki
, Hoyoung Choi
, Jae Hun Choi
, Minho Yun
, Byeong Seon Jeong
, Yurngdong Jahng
, Younghwa Na
, Won Jea Cho
, Youngjoo Kwon
, Chong Soon Lee
, Eung Seok Lee

Department of Pharmaceutical Sciences

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

52 Scopus citations

Abstract

For the development of novel antitumor agents, 2,6-dithienyl-4-furyl pyridine derivatives were prepared and evaluated for their topoisomerase I and II inhibitory activity as well as cytotoxicity against several human cancer cell lines. Among the 21 prepared compounds, compound 24 exhibited strong topoisomerase I inhibitory activity. In addition, a docking study with topoisomerase I and compound 24 was performed.

Original language	English
Pages (from-to)	42-47
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	20
Issue number	1
DOIs	https://doi.org/10.1016/j.bmcl.2009.11.041
State	Published - 1 Jan 2010

Bibliographical note

Funding Information:
This work was supported by the Korea Research Foundation Grant funded by the Korean Government (MOEHRD, Basic Research Promotion Fund) ( KRF-2008-313-E00762 ).

Keywords

2,6-Dithienyl-4-furyl pyridine
Antitumor agents
Cytotoxicity
Docking study
Topoisomerase I and II inhibitor

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10.1016/j.bmcl.2009.11.041

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Basnet, A., Thapa, P., Karki, R., Choi, H., Choi, J. H., Yun, M., Jeong, B. S., Jahng, Y., Na, Y., Cho, W. J., Kwon, Y., Lee, C. S., & Lee, E. S. (2010). 2,6-Dithienyl-4-furyl pyridines: Synthesis, topoisomerase I and II inhibition, cytotoxicity, structure-activity relationship, and docking study. Bioorganic and Medicinal Chemistry Letters, 20(1), 42-47. https://doi.org/10.1016/j.bmcl.2009.11.041

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title = "2,6-Dithienyl-4-furyl pyridines: Synthesis, topoisomerase I and II inhibition, cytotoxicity, structure-activity relationship, and docking study",

abstract = "For the development of novel antitumor agents, 2,6-dithienyl-4-furyl pyridine derivatives were prepared and evaluated for their topoisomerase I and II inhibitory activity as well as cytotoxicity against several human cancer cell lines. Among the 21 prepared compounds, compound 24 exhibited strong topoisomerase I inhibitory activity. In addition, a docking study with topoisomerase I and compound 24 was performed.",

keywords = "2,6-Dithienyl-4-furyl pyridine, Antitumor agents, Cytotoxicity, Docking study, Topoisomerase I and II inhibitor",

author = "Arjun Basnet and Pritam Thapa and Radha Karki and Hoyoung Choi and Choi, \{Jae Hun\} and Minho Yun and Jeong, \{Byeong Seon\} and Yurngdong Jahng and Younghwa Na and Cho, \{Won Jea\} and Youngjoo Kwon and Lee, \{Chong Soon\} and Lee, \{Eung Seok\}",

note = "Funding Information: This work was supported by the Korea Research Foundation Grant funded by the Korean Government (MOEHRD, Basic Research Promotion Fund) ( KRF-2008-313-E00762 ). ",

year = "2010",

month = jan,

day = "1",

doi = "10.1016/j.bmcl.2009.11.041",

language = "English",

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journal = "Bioorganic and Medicinal Chemistry Letters",

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Basnet, A, Thapa, P, Karki, R, Choi, H, Choi, JH, Yun, M, Jeong, BS, Jahng, Y, Na, Y, Cho, WJ, Kwon, Y, Lee, CS & Lee, ES 2010, '2,6-Dithienyl-4-furyl pyridines: Synthesis, topoisomerase I and II inhibition, cytotoxicity, structure-activity relationship, and docking study', Bioorganic and Medicinal Chemistry Letters, vol. 20, no. 1, pp. 42-47. https://doi.org/10.1016/j.bmcl.2009.11.041

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T1 - 2,6-Dithienyl-4-furyl pyridines

T2 - Synthesis, topoisomerase I and II inhibition, cytotoxicity, structure-activity relationship, and docking study

AU - Basnet, Arjun

AU - Thapa, Pritam

AU - Karki, Radha

AU - Choi, Hoyoung

AU - Choi, Jae Hun

AU - Yun, Minho

AU - Jeong, Byeong Seon

AU - Jahng, Yurngdong

AU - Na, Younghwa

AU - Cho, Won Jea

AU - Kwon, Youngjoo

AU - Lee, Chong Soon

AU - Lee, Eung Seok

N1 - Funding Information: This work was supported by the Korea Research Foundation Grant funded by the Korean Government (MOEHRD, Basic Research Promotion Fund) ( KRF-2008-313-E00762 ).

PY - 2010/1/1

Y1 - 2010/1/1

N2 - For the development of novel antitumor agents, 2,6-dithienyl-4-furyl pyridine derivatives were prepared and evaluated for their topoisomerase I and II inhibitory activity as well as cytotoxicity against several human cancer cell lines. Among the 21 prepared compounds, compound 24 exhibited strong topoisomerase I inhibitory activity. In addition, a docking study with topoisomerase I and compound 24 was performed.

AB - For the development of novel antitumor agents, 2,6-dithienyl-4-furyl pyridine derivatives were prepared and evaluated for their topoisomerase I and II inhibitory activity as well as cytotoxicity against several human cancer cell lines. Among the 21 prepared compounds, compound 24 exhibited strong topoisomerase I inhibitory activity. In addition, a docking study with topoisomerase I and compound 24 was performed.

KW - 2,6-Dithienyl-4-furyl pyridine

KW - Antitumor agents

KW - Cytotoxicity

KW - Docking study

KW - Topoisomerase I and II inhibitor

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M3 - Article

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SN - 0960-894X

VL - 20

SP - 42

EP - 47

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 1

ER -

2,6-Dithienyl-4-furyl pyridines: Synthesis, topoisomerase I and II inhibition, cytotoxicity, structure-activity relationship, and docking study

Abstract

Bibliographical note

Keywords

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