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

51 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,

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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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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 ).

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

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KW - Cytotoxicity

KW - Docking study

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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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