Design, synthesis and docking study of 5-amino substituted indeno[1,2-c]isoquinolines as novel topoisomerase i inhibitors

Daulat Bikram Khadka; Quynh Manh Le; Su Hui Yang; Hue Thi My Van; Thanh Nguyen Le; Suk Hee Cho; Youngjoo Kwon; Kyung Tae Lee; Eung Seok Lee; Won Jea Cho

doi:10.1016/j.bmc.2011.01.064

Design, synthesis and docking study of 5-amino substituted indeno[1,2-c]isoquinolines as novel topoisomerase i inhibitors

Daulat Bikram Khadka, Quynh Manh Le, Su Hui Yang, Hue Thi My Van, Thanh Nguyen Le, Suk Hee Cho, Youngjoo Kwon, Kyung Tae Lee, Eung Seok Lee, Won Jea Cho

Department of Pharmaceutical Sciences

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

17 Scopus citations

Abstract

Various 5-amino group-substituted indeno[1,2-c]isoquinolines 7a-f were synthesized based on the previous QSAR study as rigid structures of 3-arylisoquinolines. Amino group-substituted compounds, especially 5-piperazinyl indeno[1,2-c]isoquinoline 7f, displayed potent topoisomerase I inhibitory activity as well as cytotoxicities against five different tumor cell lines. A Surflex-Dock docking model of 7f was also studied.

Original language	English
Pages (from-to)	1924-1929
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry
Volume	19
Issue number	6
DOIs	https://doi.org/10.1016/j.bmc.2011.01.064
State	Published - 15 Mar 2011

Bibliographical note

Funding Information:
This work was supported by Korea Research Foundation grant ( KRF-2009-0071379 ).

Keywords

Cytotoxicity
Docking study
Indeno[1,2-c]isoquinolines
Topoisomerase I

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10.1016/j.bmc.2011.01.064

Cite this

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title = "Design, synthesis and docking study of 5-amino substituted indeno[1,2-c]isoquinolines as novel topoisomerase i inhibitors",

abstract = "Various 5-amino group-substituted indeno[1,2-c]isoquinolines 7a-f were synthesized based on the previous QSAR study as rigid structures of 3-arylisoquinolines. Amino group-substituted compounds, especially 5-piperazinyl indeno[1,2-c]isoquinoline 7f, displayed potent topoisomerase I inhibitory activity as well as cytotoxicities against five different tumor cell lines. A Surflex-Dock docking model of 7f was also studied.",

keywords = "Cytotoxicity, Docking study, Indeno[1,2-c]isoquinolines, Topoisomerase I",

author = "Khadka, {Daulat Bikram} and Le, {Quynh Manh} and Yang, {Su Hui} and Van, {Hue Thi My} and Le, {Thanh Nguyen} and Cho, {Suk Hee} and Youngjoo Kwon and Lee, {Kyung Tae} and Lee, {Eung Seok} and Cho, {Won Jea}",

note = "Funding Information: This work was supported by Korea Research Foundation grant ( KRF-2009-0071379 ).",

year = "2011",

month = mar,

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doi = "10.1016/j.bmc.2011.01.064",

language = "English",

volume = "19",

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journal = "Bioorganic and Medicinal Chemistry",

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T1 - Design, synthesis and docking study of 5-amino substituted indeno[1,2-c]isoquinolines as novel topoisomerase i inhibitors

AU - Khadka, Daulat Bikram

AU - Le, Quynh Manh

AU - Yang, Su Hui

AU - Van, Hue Thi My

AU - Le, Thanh Nguyen

AU - Cho, Suk Hee

AU - Kwon, Youngjoo

AU - Lee, Kyung Tae

AU - Lee, Eung Seok

AU - Cho, Won Jea

N1 - Funding Information: This work was supported by Korea Research Foundation grant ( KRF-2009-0071379 ).

PY - 2011/3/15

Y1 - 2011/3/15

N2 - Various 5-amino group-substituted indeno[1,2-c]isoquinolines 7a-f were synthesized based on the previous QSAR study as rigid structures of 3-arylisoquinolines. Amino group-substituted compounds, especially 5-piperazinyl indeno[1,2-c]isoquinoline 7f, displayed potent topoisomerase I inhibitory activity as well as cytotoxicities against five different tumor cell lines. A Surflex-Dock docking model of 7f was also studied.

AB - Various 5-amino group-substituted indeno[1,2-c]isoquinolines 7a-f were synthesized based on the previous QSAR study as rigid structures of 3-arylisoquinolines. Amino group-substituted compounds, especially 5-piperazinyl indeno[1,2-c]isoquinoline 7f, displayed potent topoisomerase I inhibitory activity as well as cytotoxicities against five different tumor cell lines. A Surflex-Dock docking model of 7f was also studied.

KW - Cytotoxicity

KW - Docking study

KW - Indeno[1,2-c]isoquinolines

KW - Topoisomerase I

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SN - 0968-0896

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JO - Bioorganic and Medicinal Chemistry

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ER -

Design, synthesis and docking study of 5-amino substituted indeno[1,2-c]isoquinolines as novel topoisomerase i inhibitors

Abstract

Bibliographical note

Keywords

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