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,

day = "15",

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

language = "English",

volume = "19",

pages = "1924--1929",

journal = "Bioorganic and Medicinal Chemistry",

issn = "0968-0896",

publisher = "Elsevier Ltd.",

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TY - JOUR

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

UR - https://www.scopus.com/pages/publications/79952442830

U2 - 10.1016/j.bmc.2011.01.064

DO - 10.1016/j.bmc.2011.01.064

M3 - Article

C2 - 21353568

AN - SCOPUS:79952442830

SN - 0968-0896

VL - 19

SP - 1924

EP - 1929

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

IS - 6

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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