Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship study of hydroxylated 2,4-diphenyl-6-aryl pyridines

Radha Karki; Pritam Thapa; Mi Jeong Kang; Tae Cheon Jeong; Jung Min Nam; Hye Lin Kim; Younghwa Na; Won Jea Cho; Youngjoo Kwon; Eung Seok Lee

doi:10.1016/j.bmc.2010.03.051

Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship study of hydroxylated 2,4-diphenyl-6-aryl pyridines

Radha Karki, Pritam Thapa, Mi Jeong Kang, Tae Cheon Jeong, Jung Min Nam, Hye Lin Kim, Younghwa Na, Won Jea Cho, Youngjoo Kwon, Eung Seok Lee

Department of Pharmaceutical Sciences

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

99 Scopus citations

Abstract

A new series of 2,4-diphenyl-6-aryl pyridines containing hydroxyl group(s) at the ortho, meta, or para position of the phenyl ring were synthesized, and evaluated for topoisomerase I and II inhibitory activity and cytotoxicity against several human cancer cell lines for the development of novel anticancer agents. Structure-activity relationship study revealed that the substitution of hydroxyl group(s) increased topoisomerase I and II inhibitory activity in the order of meta > para > ortho position. Substitution of hydroxyl group on the para position showed better cytotoxicity.

Original language	English
Pages (from-to)	3066-3077
Number of pages	12
Journal	Bioorganic and Medicinal Chemistry
Volume	18
Issue number	9
DOIs	https://doi.org/10.1016/j.bmc.2010.03.051
State	Published - 1 May 2010

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 (2010-0007620).

Keywords

Anticancer agents
Cytotoxicity
Hydroxylated 2,4-diphenyl-6-aryl pyridines
Topoisomerase I and II inhibitor

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Karki, R., Thapa, P., Kang, M. J., Jeong, T. C., Nam, J. M., Kim, H. L., Na, Y., Cho, W. J., Kwon, Y., & Lee, E. S. (2010). Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship study of hydroxylated 2,4-diphenyl-6-aryl pyridines. Bioorganic and Medicinal Chemistry, 18(9), 3066-3077. https://doi.org/10.1016/j.bmc.2010.03.051

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title = "Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship study of hydroxylated 2,4-diphenyl-6-aryl pyridines",

abstract = "A new series of 2,4-diphenyl-6-aryl pyridines containing hydroxyl group(s) at the ortho, meta, or para position of the phenyl ring were synthesized, and evaluated for topoisomerase I and II inhibitory activity and cytotoxicity against several human cancer cell lines for the development of novel anticancer agents. Structure-activity relationship study revealed that the substitution of hydroxyl group(s) increased topoisomerase I and II inhibitory activity in the order of meta > para > ortho position. Substitution of hydroxyl group on the para position showed better cytotoxicity.",

keywords = "Anticancer agents, Cytotoxicity, Hydroxylated 2,4-diphenyl-6-aryl pyridines, Topoisomerase I and II inhibitor",

author = "Radha Karki and Pritam Thapa and Kang, {Mi Jeong} and Jeong, {Tae Cheon} and Nam, {Jung Min} and Kim, {Hye Lin} and Younghwa Na 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 (2010-0007620).",

year = "2010",

month = may,

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doi = "10.1016/j.bmc.2010.03.051",

language = "English",

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journal = "Bioorganic and Medicinal Chemistry",

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AU - Karki, Radha

AU - Thapa, Pritam

AU - Kang, Mi Jeong

AU - Jeong, Tae Cheon

AU - Nam, Jung Min

AU - Kim, Hye Lin

AU - Na, Younghwa

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 (2010-0007620).

PY - 2010/5/1

Y1 - 2010/5/1

N2 - A new series of 2,4-diphenyl-6-aryl pyridines containing hydroxyl group(s) at the ortho, meta, or para position of the phenyl ring were synthesized, and evaluated for topoisomerase I and II inhibitory activity and cytotoxicity against several human cancer cell lines for the development of novel anticancer agents. Structure-activity relationship study revealed that the substitution of hydroxyl group(s) increased topoisomerase I and II inhibitory activity in the order of meta > para > ortho position. Substitution of hydroxyl group on the para position showed better cytotoxicity.

AB - A new series of 2,4-diphenyl-6-aryl pyridines containing hydroxyl group(s) at the ortho, meta, or para position of the phenyl ring were synthesized, and evaluated for topoisomerase I and II inhibitory activity and cytotoxicity against several human cancer cell lines for the development of novel anticancer agents. Structure-activity relationship study revealed that the substitution of hydroxyl group(s) increased topoisomerase I and II inhibitory activity in the order of meta > para > ortho position. Substitution of hydroxyl group on the para position showed better cytotoxicity.

KW - Anticancer agents

KW - Cytotoxicity

KW - Hydroxylated 2,4-diphenyl-6-aryl pyridines

KW - Topoisomerase I and II inhibitor

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DO - 10.1016/j.bmc.2010.03.051

M3 - Article

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AN - SCOPUS:77951204579

SN - 0968-0896

VL - 18

SP - 3066

EP - 3077

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

IS - 9

ER -

Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship study of hydroxylated 2,4-diphenyl-6-aryl pyridines

Abstract

Bibliographical note

Keywords

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