2,4-Diaryl-5,6-dihydro-1,10-phenanthroline and 2,4-diaryl-5,6- dihydrothieno[2,3-h] quinoline derivatives for topoisomerase i and II inhibitory activity, cytotoxicity, and structure-activity relationship study

Pritam Thapa; Radha Karki; Han Young Yoo; Pil Hoon Park; Eunyoung Lee; Kyung Hwa Jeon; Younghwa Na; Won Jea Cho; Youngjoo Kwon; Eung Seok Lee

doi:10.1016/j.bioorg.2011.09.001

2,4-Diaryl-5,6-dihydro-1,10-phenanthroline and 2,4-diaryl-5,6- dihydrothieno[2,3-h] quinoline derivatives for topoisomerase i and II inhibitory activity, cytotoxicity, and structure-activity relationship study

Pritam Thapa, Radha Karki, Han Young Yoo, Pil Hoon Park, Eunyoung Lee, Kyung Hwa Jeon, Younghwa Na, Won Jea Cho, Youngjoo Kwon, Eung Seok Lee

Department of Pharmaceutical Sciences

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

24 Scopus citations

Abstract

Designed and synthesized thirty-two 2,4-diaryl-5,6-dihydro-1,10- phenanthroline and 2,4-diaryl-5,6-dihydrothieno[2,3-h] quinoline derivatives as rigid analogs of 2,4,6-trisubstituted pyridines were evaluated for topoisomerase I and II inhibitory activities as well as cytotoxicities against several human cancer cell lines. Structure-activity relationship study showed that [2,2′;6′,2″]-terpyridine skeleton is important for the cytotoxicity against several human cancer cell lines.

Original language	English
Pages (from-to)	67-78
Number of pages	12
Journal	Bioorganic Chemistry
Volume	40
Issue number	1
DOIs	https://doi.org/10.1016/j.bioorg.2011.09.001
State	Published - Feb 2012

Bibliographical note

Funding Information:
This work was supported by the 2011 Yeungnam University Research Grant.

Keywords

2,4-Diaryl-5,6- dihydrothieno[2,3-h] quinoline
2,4-Diaryl-5,6-dihydro-1,10-phenanthroline
Cytotoxicity
Terpyridine
Topoisomerase I and II

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Thapa, P., Karki, R., Yoo, H. Y., Park, P. H., Lee, E., Jeon, K. H., Na, Y., Cho, W. J., Kwon, Y., & Lee, E. S. (2012). 2,4-Diaryl-5,6-dihydro-1,10-phenanthroline and 2,4-diaryl-5,6- dihydrothieno[2,3-h] quinoline derivatives for topoisomerase i and II inhibitory activity, cytotoxicity, and structure-activity relationship study. Bioorganic Chemistry, 40(1), 67-78. https://doi.org/10.1016/j.bioorg.2011.09.001

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title = "2,4-Diaryl-5,6-dihydro-1,10-phenanthroline and 2,4-diaryl-5,6- dihydrothieno[2,3-h] quinoline derivatives for topoisomerase i and II inhibitory activity, cytotoxicity, and structure-activity relationship study",

abstract = "Designed and synthesized thirty-two 2,4-diaryl-5,6-dihydro-1,10- phenanthroline and 2,4-diaryl-5,6-dihydrothieno[2,3-h] quinoline derivatives as rigid analogs of 2,4,6-trisubstituted pyridines were evaluated for topoisomerase I and II inhibitory activities as well as cytotoxicities against several human cancer cell lines. Structure-activity relationship study showed that [2,2′;6′,2″]-terpyridine skeleton is important for the cytotoxicity against several human cancer cell lines.",

keywords = "2,4-Diaryl-5,6- dihydrothieno[2,3-h] quinoline, 2,4-Diaryl-5,6-dihydro-1,10-phenanthroline, Cytotoxicity, Terpyridine, Topoisomerase I and II",

author = "Pritam Thapa and Radha Karki and Yoo, {Han Young} and Park, {Pil Hoon} and Eunyoung Lee and Jeon, {Kyung Hwa} and Younghwa Na and Cho, {Won Jea} and Youngjoo Kwon and Lee, {Eung Seok}",

note = "Funding Information: This work was supported by the 2011 Yeungnam University Research Grant.",

year = "2012",

month = feb,

doi = "10.1016/j.bioorg.2011.09.001",

language = "English",

volume = "40",

pages = "67--78",

journal = "Bioorganic Chemistry",

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Thapa, P, Karki, R, Yoo, HY, Park, PH, Lee, E, Jeon, KH, Na, Y, Cho, WJ, Kwon, Y & Lee, ES 2012, '2,4-Diaryl-5,6-dihydro-1,10-phenanthroline and 2,4-diaryl-5,6- dihydrothieno[2,3-h] quinoline derivatives for topoisomerase i and II inhibitory activity, cytotoxicity, and structure-activity relationship study', Bioorganic Chemistry, vol. 40, no. 1, pp. 67-78. https://doi.org/10.1016/j.bioorg.2011.09.001

2,4-Diaryl-5,6-dihydro-1,10-phenanthroline and 2,4-diaryl-5,6- dihydrothieno[2,3-h] quinoline derivatives for topoisomerase i and II inhibitory activity, cytotoxicity, and structure-activity relationship study. / Thapa, Pritam; Karki, Radha; Yoo, Han Young et al.
In: Bioorganic Chemistry, Vol. 40, No. 1, 02.2012, p. 67-78.

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

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AU - Thapa, Pritam

AU - Karki, Radha

AU - Yoo, Han Young

AU - Park, Pil Hoon

AU - Lee, Eunyoung

AU - Jeon, Kyung Hwa

AU - Na, Younghwa

AU - Cho, Won Jea

AU - Kwon, Youngjoo

AU - Lee, Eung Seok

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AB - Designed and synthesized thirty-two 2,4-diaryl-5,6-dihydro-1,10- phenanthroline and 2,4-diaryl-5,6-dihydrothieno[2,3-h] quinoline derivatives as rigid analogs of 2,4,6-trisubstituted pyridines were evaluated for topoisomerase I and II inhibitory activities as well as cytotoxicities against several human cancer cell lines. Structure-activity relationship study showed that [2,2′;6′,2″]-terpyridine skeleton is important for the cytotoxicity against several human cancer cell lines.

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KW - Cytotoxicity

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