Dihydroxylated 2,4,6-triphenyl pyridines: Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure–activity relationship study
Radha Karki
1
,
Pritam Thapa
1
,
Han Wook Yoo
1
,
Tara Man Kadayat
1
,
Pil-Hoon Park
1
,
Youngwha Na
2
,
Yong-Ho Lee
3
,
Kyung Neoyh Jeon
3
,
W S Cho
4
,
Heesung Choi
5
,
Youngjoo Kwon
3
,
Eung Ho Lee
1
5
Eli Lilly Korea Ltd., Seoul 100-958, Republic of Korea
|
Publication type: Journal Article
Publication date: 2012-03-01
scimago Q1
wos Q1
SJR: 1.142
CiteScore: 11.3
Impact factor: 5.9
ISSN: 02235234, 17683254
PubMed ID:
22318164
Organic Chemistry
Drug Discovery
General Medicine
Pharmacology
Abstract
Twelve dihydroxylated 2,4,6-triphenyl pyridines were designed and synthesized which contain hydroxyl groups at ortho, meta or para position of 2- and 6-phenyl, or 2- and 4-phenyl rings attached to the central pyridine. They were evaluated for topoisomerase I and II inhibitory activity, and cytotoxicity against several human cancer cell lines for the development of novel anticancer agents. Generally, dihydroxylated 2,4,6-triphenyl pyridines exhibited stronger topoisomerase II inhibitory activity, and cytotoxicity compared to those of monohydroxylated 2,4,6-triphenyl pyridines. The concrete structure-activity relationship was observed that dihydroxylated 2,4,6-triphenyl pyridines with hydroxyl group at meta or para position of 2-phenyl ring displayed significant topoisomerase II inhibitory activity as well as cytotoxicity. Positive correlation between topoisomerase II inhibitory activity and cytotoxicity was observed for compounds 10, 12, 13, 17-20 and 22.
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Total citations:
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Citations from 2025:
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(1.41%)
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GOST
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Karki R. et al. Dihydroxylated 2,4,6-triphenyl pyridines: Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure–activity relationship study // European Journal of Medicinal Chemistry. 2012. Vol. 49. pp. 219-228.
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Karki R., Thapa P., Yoo H. W., Kadayat T. M., Park P., Na Y., Lee Y., Jeon K. N., Cho W. S., Choi H., Kwon Y., Lee E. H. Dihydroxylated 2,4,6-triphenyl pyridines: Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure–activity relationship study // European Journal of Medicinal Chemistry. 2012. Vol. 49. pp. 219-228.
Cite this
RIS
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TY - JOUR
DO - 10.1016/j.ejmech.2012.01.015
UR - https://doi.org/10.1016/j.ejmech.2012.01.015
TI - Dihydroxylated 2,4,6-triphenyl pyridines: Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure–activity relationship study
T2 - European Journal of Medicinal Chemistry
AU - Karki, Radha
AU - Thapa, Pritam
AU - Yoo, Han Wook
AU - Kadayat, Tara Man
AU - Park, Pil-Hoon
AU - Na, Youngwha
AU - Lee, Yong-Ho
AU - Jeon, Kyung Neoyh
AU - Cho, W S
AU - Choi, Heesung
AU - Kwon, Youngjoo
AU - Lee, Eung Ho
PY - 2012
DA - 2012/03/01
PB - Elsevier
SP - 219-228
VL - 49
PMID - 22318164
SN - 0223-5234
SN - 1768-3254
ER -
Cite this
BibTex (up to 50 authors)
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@article{2012_Karki,
author = {Radha Karki and Pritam Thapa and Han Wook Yoo and Tara Man Kadayat and Pil-Hoon Park and Youngwha Na and Yong-Ho Lee and Kyung Neoyh Jeon and W S Cho and Heesung Choi and Youngjoo Kwon and Eung Ho Lee},
title = {Dihydroxylated 2,4,6-triphenyl pyridines: Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure–activity relationship study},
journal = {European Journal of Medicinal Chemistry},
year = {2012},
volume = {49},
publisher = {Elsevier},
month = {mar},
url = {https://doi.org/10.1016/j.ejmech.2012.01.015},
pages = {219--228},
doi = {10.1016/j.ejmech.2012.01.015}
}