2-Chlorophenyl-substituted benzofuro[3,2-b]pyridines with enhanced topoisomerase inhibitory activity: The role of the chlorine substituent

Til Bahadur Thapa Magar; Tara Man Kadayat; Hwa Jong Lee; Seojeong Park; Ganesh Bist; Aarajana Shrestha; Youngjoo Kwon; Eung Seok Lee

doi:10.1016/j.bmcl.2017.06.025

2-Chlorophenyl-substituted benzofuro[3,2-b]pyridines with enhanced topoisomerase inhibitory activity: The role of the chlorine substituent

Til Bahadur Thapa Magar
, Tara Man Kadayat
, Hwa Jong Lee
, Seojeong Park
, Ganesh Bist
, Aarajana Shrestha
, Youngjoo Kwon
, Eung Seok Lee

Department of Pharmaceutical Sciences

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

22 Scopus citations

Abstract

A new series of 2-chloropheny-substituted benzofuro[3,2-b]pyridines were designed, synthesized, and evaluated for topoisomerase I and II inhibition and antiproliferative activity. Compounds 17–19, 23, 24, 26, and 27 exhibited excellent topo II inhibitory activity. A systematic structure-activity relationship study revealed the important role of chlorine substitution in the strong topoisomerase inhibitory activity.

Original language	English
Pages (from-to)	3279-3283
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	27
Issue number	15
DOIs	https://doi.org/10.1016/j.bmcl.2017.06.025
State	Published - 2017

Bibliographical note

Publisher Copyright:
© 2017 Elsevier Ltd

Keywords

Antiproliferative activity
Benzofuro[3,2-b]pyridines
Chlorine-substituent
Heterocycles
Topoisomerase I and II inhibition

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10.1016/j.bmcl.2017.06.025

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title = "2-Chlorophenyl-substituted benzofuro[3,2-b]pyridines with enhanced topoisomerase inhibitory activity: The role of the chlorine substituent",

abstract = "A new series of 2-chloropheny-substituted benzofuro[3,2-b]pyridines were designed, synthesized, and evaluated for topoisomerase I and II inhibition and antiproliferative activity. Compounds 17–19, 23, 24, 26, and 27 exhibited excellent topo II inhibitory activity. A systematic structure-activity relationship study revealed the important role of chlorine substitution in the strong topoisomerase inhibitory activity.",

keywords = "Antiproliferative activity, Benzofuro[3,2-b]pyridines, Chlorine-substituent, Heterocycles, Topoisomerase I and II inhibition",

author = "\{Thapa Magar\}, \{Til Bahadur\} and Kadayat, \{Tara Man\} and Lee, \{Hwa Jong\} and Seojeong Park and Ganesh Bist and Aarajana Shrestha and Youngjoo Kwon and Lee, \{Eung Seok\}",

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year = "2017",

doi = "10.1016/j.bmcl.2017.06.025",

language = "English",

volume = "27",

pages = "3279--3283",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

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}

TY - JOUR

T1 - 2-Chlorophenyl-substituted benzofuro[3,2-b]pyridines with enhanced topoisomerase inhibitory activity

T2 - The role of the chlorine substituent

AU - Thapa Magar, Til Bahadur

AU - Kadayat, Tara Man

AU - Lee, Hwa Jong

AU - Park, Seojeong

AU - Bist, Ganesh

AU - Shrestha, Aarajana

AU - Kwon, Youngjoo

AU - Lee, Eung Seok

PY - 2017

Y1 - 2017

N2 - A new series of 2-chloropheny-substituted benzofuro[3,2-b]pyridines were designed, synthesized, and evaluated for topoisomerase I and II inhibition and antiproliferative activity. Compounds 17–19, 23, 24, 26, and 27 exhibited excellent topo II inhibitory activity. A systematic structure-activity relationship study revealed the important role of chlorine substitution in the strong topoisomerase inhibitory activity.

AB - A new series of 2-chloropheny-substituted benzofuro[3,2-b]pyridines were designed, synthesized, and evaluated for topoisomerase I and II inhibition and antiproliferative activity. Compounds 17–19, 23, 24, 26, and 27 exhibited excellent topo II inhibitory activity. A systematic structure-activity relationship study revealed the important role of chlorine substitution in the strong topoisomerase inhibitory activity.

KW - Antiproliferative activity

KW - Benzofuro[3,2-b]pyridines

KW - Chlorine-substituent

KW - Heterocycles

KW - Topoisomerase I and II inhibition

UR - https://www.scopus.com/pages/publications/85020548858

U2 - 10.1016/j.bmcl.2017.06.025

DO - 10.1016/j.bmcl.2017.06.025

M3 - Article

C2 - 28633898

AN - SCOPUS:85020548858

SN - 0960-894X

VL - 27

SP - 3279

EP - 3283

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 15

ER -

2-Chlorophenyl-substituted benzofuro[3,2-b]pyridines with enhanced topoisomerase inhibitory activity: The role of the chlorine substituent

Abstract

Bibliographical note

Keywords

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