Synthesis and antitumor activity of 4-hydroxycoumarin derivatives

Jae Chul Jung; Ji Ho Lee; Seikwan Oh; Jae Gon Lee; Oee Sook Park

doi:10.1016/j.bmcl.2004.09.009

Synthesis and antitumor activity of 4-hydroxycoumarin derivatives

Jae Chul Jung, Ji Ho Lee, Seikwan Oh, Jae Gon Lee, Oee Sook Park

Department of Molecular Medicine

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

93 Scopus citations

Abstract

A series of 4-hydroxycoumarin derivatives was prepared and evaluated for antitumor activity against five human tumor cell lines. A series of 4-hydroxycoumarin derivatives was prepared and evaluated for antitumor activity. The key fragments were 2a-c, 5c, 12b, 13b, 17, and 18 which were prepared via dianion ring cyclization, Friedel-Crafts acylation, and Reformatsky reaction. Compound 20b showed the most potent antitumor activity among the total 12 derivatives and compounds 19a and 19b exhibited efficacy comparable to etoposide in vitro antitumor activity.

Original language	English
Pages (from-to)	5527-5531
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	14
Issue number	22
DOIs	https://doi.org/10.1016/j.bmcl.2004.09.009
State	Published - 15 Nov 2004

Bibliographical note

Funding Information:
This work has been supported by Chungbuk National University Grant in 2004. We would like to thank Dr. Kimberly K. Vines for consideration of this manuscript.

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10.1016/j.bmcl.2004.09.009

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title = "Synthesis and antitumor activity of 4-hydroxycoumarin derivatives",

abstract = "A series of 4-hydroxycoumarin derivatives was prepared and evaluated for antitumor activity against five human tumor cell lines. A series of 4-hydroxycoumarin derivatives was prepared and evaluated for antitumor activity. The key fragments were 2a-c, 5c, 12b, 13b, 17, and 18 which were prepared via dianion ring cyclization, Friedel-Crafts acylation, and Reformatsky reaction. Compound 20b showed the most potent antitumor activity among the total 12 derivatives and compounds 19a and 19b exhibited efficacy comparable to etoposide in vitro antitumor activity.",

author = "Jung, {Jae Chul} and Lee, {Ji Ho} and Seikwan Oh and Lee, {Jae Gon} and Park, {Oee Sook}",

note = "Funding Information: This work has been supported by Chungbuk National University Grant in 2004. We would like to thank Dr. Kimberly K. Vines for consideration of this manuscript. ",

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T1 - Synthesis and antitumor activity of 4-hydroxycoumarin derivatives

AU - Jung, Jae Chul

AU - Lee, Ji Ho

AU - Oh, Seikwan

AU - Lee, Jae Gon

AU - Park, Oee Sook

N1 - Funding Information: This work has been supported by Chungbuk National University Grant in 2004. We would like to thank Dr. Kimberly K. Vines for consideration of this manuscript.

PY - 2004/11/15

Y1 - 2004/11/15

N2 - A series of 4-hydroxycoumarin derivatives was prepared and evaluated for antitumor activity against five human tumor cell lines. A series of 4-hydroxycoumarin derivatives was prepared and evaluated for antitumor activity. The key fragments were 2a-c, 5c, 12b, 13b, 17, and 18 which were prepared via dianion ring cyclization, Friedel-Crafts acylation, and Reformatsky reaction. Compound 20b showed the most potent antitumor activity among the total 12 derivatives and compounds 19a and 19b exhibited efficacy comparable to etoposide in vitro antitumor activity.

AB - A series of 4-hydroxycoumarin derivatives was prepared and evaluated for antitumor activity against five human tumor cell lines. A series of 4-hydroxycoumarin derivatives was prepared and evaluated for antitumor activity. The key fragments were 2a-c, 5c, 12b, 13b, 17, and 18 which were prepared via dianion ring cyclization, Friedel-Crafts acylation, and Reformatsky reaction. Compound 20b showed the most potent antitumor activity among the total 12 derivatives and compounds 19a and 19b exhibited efficacy comparable to etoposide in vitro antitumor activity.

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SN - 0960-894X

VL - 14

SP - 5527

EP - 5531

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 22

ER -

Synthesis and antitumor activity of 4-hydroxycoumarin derivatives

Abstract

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