Synthesis and antiproliferative activity of pyrrolo[3,2-b]pyridine derivatives against melanoma

Hee Jin Kim; Myung Ho Jung; Hwan Kim; Mohammed I. El-Gamal; Tae Bo Sim; So Ha Lee; Jun Hee Hong; Jung Mi Hah; Jung Hyuck Cho; Jung Hoon Choi; Kyung Ho Yoo; Chang Hyun Oh

doi:10.1016/j.bmcl.2009.08.005

Synthesis and antiproliferative activity of pyrrolo[3,2-b]pyridine derivatives against melanoma

Hee Jin Kim, Myung Ho Jung, Hwan Kim, Mohammed I. El-Gamal, Tae Bo Sim, So Ha Lee, Jun Hee Hong, Jung Mi Hah, Jung Hyuck Cho, Jung Hoon Choi, Kyung Ho Yoo, Chang Hyun Oh

KU-KIST Graduate School of Converging Science and Technology

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

37 Citations (Scopus)

Abstract

Synthesis of a new series of diarylureas and amides having pyrrolo[3,2-b]pyridine scaffold is described. Their in vitro antiproliferative activity against human melanoma cell line A375 and HS 27 human fibroblast cell line was tested and the effect of substituents on the pyrrolo[3,2-b]pyridine was investigated. The newly synthesized compounds, except meta-substituted derivatives (Ij-k and Iv-w), generally showed superior or similar activity against A375 to Sorafenib. Among all of these derivatives, compounds Ir and It having 5-benzylamide substituted 4′-amide moieties showed the most potent antiproliferative activity against A375.

Original language	English
Pages (from-to)	413-417
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	20
Issue number	1
DOIs	https://doi.org/10.1016/j.bmcl.2009.08.005
Publication status	Published - 2010 Jan 1

Keywords

A375
Antiproliferative activity
HS 27
Melanoma
Pyrrolo[3,2-b]pyridine

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/j.bmcl.2009.08.005

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title = "Synthesis and antiproliferative activity of pyrrolo[3,2-b]pyridine derivatives against melanoma",

abstract = "Synthesis of a new series of diarylureas and amides having pyrrolo[3,2-b]pyridine scaffold is described. Their in vitro antiproliferative activity against human melanoma cell line A375 and HS 27 human fibroblast cell line was tested and the effect of substituents on the pyrrolo[3,2-b]pyridine was investigated. The newly synthesized compounds, except meta-substituted derivatives (Ij-k and Iv-w), generally showed superior or similar activity against A375 to Sorafenib. Among all of these derivatives, compounds Ir and It having 5-benzylamide substituted 4′-amide moieties showed the most potent antiproliferative activity against A375.",

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doi = "10.1016/j.bmcl.2009.08.005",

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AU - Kim, Hee Jin

AU - Jung, Myung Ho

AU - Kim, Hwan

AU - El-Gamal, Mohammed I.

AU - Sim, Tae Bo

AU - Lee, So Ha

AU - Hong, Jun Hee

AU - Hah, Jung Mi

AU - Cho, Jung Hyuck

AU - Choi, Jung Hoon

AU - Yoo, Kyung Ho

AU - Oh, Chang Hyun

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AB - Synthesis of a new series of diarylureas and amides having pyrrolo[3,2-b]pyridine scaffold is described. Their in vitro antiproliferative activity against human melanoma cell line A375 and HS 27 human fibroblast cell line was tested and the effect of substituents on the pyrrolo[3,2-b]pyridine was investigated. The newly synthesized compounds, except meta-substituted derivatives (Ij-k and Iv-w), generally showed superior or similar activity against A375 to Sorafenib. Among all of these derivatives, compounds Ir and It having 5-benzylamide substituted 4′-amide moieties showed the most potent antiproliferative activity against A375.

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KW - Antiproliferative activity

KW - HS 27

KW - Melanoma

KW - Pyrrolo[3,2-b]pyridine

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Synthesis and antiproliferative activity of pyrrolo[3,2-b]pyridine derivatives against melanoma

Abstract

Keywords

ASJC Scopus subject areas

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