Synthesis of 2,4-diaryl chromenopyridines and evaluation of their topoisomerase i and II inhibitory activity, cytotoxicity, and structure-activity relationship

Uttam Thapa; Pritam Thapa; Radha Karki; Minho Yun; Jae Hun Choi; Yurngdong Jahng; Eunyoung Lee; Kyung Hwa Jeon; Younghwa Na; Eun Mi Ha; Won Jea Cho; Youngjoo Kwon; Eung Seok Lee

doi:10.1016/j.ejmech.2011.04.029

Synthesis of 2,4-diaryl chromenopyridines and evaluation of their topoisomerase i and II inhibitory activity, cytotoxicity, and structure-activity relationship

Uttam Thapa, Pritam Thapa, Radha Karki, Minho Yun, Jae Hun Choi, Yurngdong Jahng, Eunyoung Lee, Kyung Hwa Jeon, Younghwa Na, Eun Mi Ha, Won Jea Cho, Youngjoo Kwon, Eung Seok Lee

Department of Pharmaceutical Sciences

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

57 Scopus citations

Abstract

Designed and synthesized were a series of 5H-chromeno[4,3-b]pyridines with substitution at 2- and 4-positions with various 5- or 6-membered heteroaromatics as antitumor agents. They 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-furyl or 2-thienyl at 2- or 4-position of central pyridine is crucial in displaying topo I or II inhibitory activity and cytotoxicity.

Original language	English
Pages (from-to)	3201-3209
Number of pages	9
Journal	European Journal of Medicinal Chemistry
Volume	46
Issue number	8
DOIs	https://doi.org/10.1016/j.ejmech.2011.04.029
State	Published - Aug 2011

Bibliographical note

Funding Information:
This research was supported by Basic Science Research Program through the National Research Foundation of Korea (NRF) funded by the Ministry of Education, Science and Technology ( 2010-0001661 , 2009-0066925 , 2010-0005506 and 2010-0002646 ).

Keywords

4-chromanone
Cytotoxicity
Terpyridine
Terthiophene
Topoisomerase I and II

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10.1016/j.ejmech.2011.04.029

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Thapa, U., Thapa, P., Karki, R., Yun, M., Choi, J. H., Jahng, Y., Lee, E., Jeon, K. H., Na, Y., Ha, E. M., Cho, W. J., Kwon, Y., & Lee, E. S. (2011). Synthesis of 2,4-diaryl chromenopyridines and evaluation of their topoisomerase i and II inhibitory activity, cytotoxicity, and structure-activity relationship. European Journal of Medicinal Chemistry, 46(8), 3201-3209. https://doi.org/10.1016/j.ejmech.2011.04.029

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title = "Synthesis of 2,4-diaryl chromenopyridines and evaluation of their topoisomerase i and II inhibitory activity, cytotoxicity, and structure-activity relationship",

abstract = "Designed and synthesized were a series of 5H-chromeno[4,3-b]pyridines with substitution at 2- and 4-positions with various 5- or 6-membered heteroaromatics as antitumor agents. They 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-furyl or 2-thienyl at 2- or 4-position of central pyridine is crucial in displaying topo I or II inhibitory activity and cytotoxicity.",

keywords = "4-chromanone, Cytotoxicity, Terpyridine, Terthiophene, Topoisomerase I and II",

author = "Uttam Thapa and Pritam Thapa and Radha Karki and Minho Yun and Choi, {Jae Hun} and Yurngdong Jahng and Eunyoung Lee and Jeon, {Kyung Hwa} and Younghwa Na and Ha, {Eun Mi} and Cho, {Won Jea} and Youngjoo Kwon and Lee, {Eung Seok}",

note = "Funding Information: This research was supported by Basic Science Research Program through the National Research Foundation of Korea (NRF) funded by the Ministry of Education, Science and Technology ( 2010-0001661 , 2009-0066925 , 2010-0005506 and 2010-0002646 ).",

year = "2011",

month = aug,

doi = "10.1016/j.ejmech.2011.04.029",

language = "English",

volume = "46",

pages = "3201--3209",

journal = "European Journal of Medicinal Chemistry",

issn = "0223-5234",

publisher = "Elsevier Masson s.r.l.",

number = "8",

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Thapa, U, Thapa, P, Karki, R, Yun, M, Choi, JH, Jahng, Y, Lee, E, Jeon, KH, Na, Y, Ha, EM, Cho, WJ, Kwon, Y & Lee, ES 2011, 'Synthesis of 2,4-diaryl chromenopyridines and evaluation of their topoisomerase i and II inhibitory activity, cytotoxicity, and structure-activity relationship', European Journal of Medicinal Chemistry, vol. 46, no. 8, pp. 3201-3209. https://doi.org/10.1016/j.ejmech.2011.04.029

TY - JOUR

T1 - Synthesis of 2,4-diaryl chromenopyridines and evaluation of their topoisomerase i and II inhibitory activity, cytotoxicity, and structure-activity relationship

AU - Thapa, Uttam

AU - Thapa, Pritam

AU - Karki, Radha

AU - Yun, Minho

AU - Choi, Jae Hun

AU - Jahng, Yurngdong

AU - Lee, Eunyoung

AU - Jeon, Kyung Hwa

AU - Na, Younghwa

AU - Ha, Eun Mi

AU - Cho, Won Jea

AU - Kwon, Youngjoo

AU - Lee, Eung Seok

N1 - Funding Information: This research was supported by Basic Science Research Program through the National Research Foundation of Korea (NRF) funded by the Ministry of Education, Science and Technology ( 2010-0001661 , 2009-0066925 , 2010-0005506 and 2010-0002646 ).

PY - 2011/8

Y1 - 2011/8

N2 - Designed and synthesized were a series of 5H-chromeno[4,3-b]pyridines with substitution at 2- and 4-positions with various 5- or 6-membered heteroaromatics as antitumor agents. They 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-furyl or 2-thienyl at 2- or 4-position of central pyridine is crucial in displaying topo I or II inhibitory activity and cytotoxicity.

AB - Designed and synthesized were a series of 5H-chromeno[4,3-b]pyridines with substitution at 2- and 4-positions with various 5- or 6-membered heteroaromatics as antitumor agents. They 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-furyl or 2-thienyl at 2- or 4-position of central pyridine is crucial in displaying topo I or II inhibitory activity and cytotoxicity.

KW - 4-chromanone

KW - Cytotoxicity

KW - Terpyridine

KW - Terthiophene

KW - Topoisomerase I and II

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SN - 0223-5234

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JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

IS - 8

ER -

Synthesis of 2,4-diaryl chromenopyridines and evaluation of their topoisomerase i and II inhibitory activity, cytotoxicity, and structure-activity relationship

Abstract

Bibliographical note

Keywords

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