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

104 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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10.1016/j.bmc.2010.03.051

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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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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

UR - https://www.scopus.com/pages/publications/77951204579

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DO - 10.1016/j.bmc.2010.03.051

M3 - Article

C2 - 20392646

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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